263 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
Roche Bioscience
Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT
Universit£
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists ofa1-adrenoceptor.
University of Bras£Lia
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea
Chinese Academy of Sciences
Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibition by Optimization of the 2-Aminopyridine-Based Scaffold with a Pyridine Linker.
Northwestern University
Design, Synthesis, and Biological Evaluation of Indoline and Indole Derivatives as Potent and Selectivea1A-Adrenoceptor Antagonists.
Chengdu University
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.
Takeda Pharmaceutical
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Indolylpiperidine derivatives as potent and selectivea1B adrenoceptor antagonists.
Toray Industries
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Humanß3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.
Asahi Kasei Pharma
Human alpha1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines.
Unsw Australia
Structure-affinity/activity relationships of 1,4-dioxa-spiro[4.5]decane based ligands ata<alpha>1 and 5-HT1A receptors.
Universit£
2-Aminopyridines with a Truncated Side Chain To Improve Human Neuronal Nitric Oxide Synthase Inhibitory Potency and Selectivity.
Northwestern University
Discovery of Quinazoline-Based Fluorescent Probes toa1-Adrenergic Receptors.
Shandong University
Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.
Northwestern University
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
High affinity ligands and potent antagonists for thea1D-adrenergic receptor. Novel 3,8-disubstituted [1]benzothieno[3,2-d]pyrimidine derivatives.
Universit£
Nitric oxide synthase inhibitors that interact with both heme propionate and tetrahydrobiopterin show high isoform selectivity.
Northwestern University
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives ina1-adrenergic and 5-HT1A receptor binding sites recognition.
University of Camerino
Target- and mechanism-based therapeutics for neurodegenerative diseases: strength in numbers.
Northwestern University
Biotransformation of LASSBio-579 and pharmacological evaluation of p-hydroxylated metabolite a N-phenylpiperazine antipsychotic lead compound.
Universidade Federal De Goi£S
Discovery of novela1-adrenoceptor ligands based on the antipsychotic sertindole suitable for labeling as PET ligands.
H. Lundbeck
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: alpha1a subtype selective 2'-heteroaryl compounds.
Glaxosmithkline
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
Glaxosmithkline
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
Glaxosmithkline
Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.
Glaxosmithkline
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
Glaxosmithkline
Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergica1- and serotonine 5-HT1A receptors.
Universit£
From libraries to candidate: the discovery of new ultra long-acting dibasicß2-adrenoceptor agonists.
Astrazeneca
Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.
Nycomed
Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands fora1-adrenoceptor subtypes.
Universit£
Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novela1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, anda1d computational study.
Universit£
1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Universit£
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
University of Camerino
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
Universit£
WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).
Universit£
Discovery of a potent, orally bioavailable and highly selective human neuronal nitric oxide synthase (nNOS) inhibitor, N-(1-(piperidin-4-yl)indolin-5-yl)thiophene-2-carboximidamide as a pre-clinical development candidate for the treatment of migraine.
Neuraxon
Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.
Sanford-Burnham Medical Research Institute
1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate.
Neuraxon
Affinity and activity profiling of unichiral 8-substituted 1,4-benzodioxane analogues of WB4101 reveals a potent and selectivea1B-adrenoceptor antagonist.
Universit£
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with µ-Opioid Agonist Activity.
TBA
First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.
Neuraxon
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
National Institute of Mental Health
Novel, druglike 1,7-disubstituted 2,3,4,5-tetrahydro-1H-benzo[b]azepine-based selective inhibitors of human neuronal nitric oxide synthase (nNOS).
Neuraxon
Discovery of N-(3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-6-yl) thiophene-2-carboximidamide as a selective inhibitor of human neuronal nitric oxide synthase (nNOS) for the treatment of pain.
Neuraxon
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging.
National Institute of Mental Health
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Hunter College and The Graduate Center of The City University of New York
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
European Research Centre For Drug Discovery and Development (Natsyndrugs)
Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Pfizer
N(delta)-Methylated L-arginine derivatives and their effects on the nitric oxide generating system.
Christian-Albrechts-University of Kiel
6-Acetyl-7,7-dimethyl-5,6,7,8-tetrahydropterin is an activator of nitric oxide synthases.
University of Strathclyde
Novel 2-aminobenzothiazoles as selective neuronal nitric oxide synthase inhibitors.
Neuraxon
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Universit£
Evaluation of pyrrolidin-2-imines and 1,3-thiazolidin-2-imines as inhibitors of nitric oxide synthase.
Merck Research Laboratory
Substituted 6-phenyl-pyridin-2-ylamines: selective and potent inhibitors of neuronal nitric oxide synthase.
Pfizer
5-Fluorinated L-lysine analogues as selective induced nitric oxide synthase inhibitors.
Pfizer
1,2-Dihydro-4-quinazolinamines: potent, highly selective inhibitors of inducible nitric oxide synthase which show antiinflammatory activity in vivo.
Astrazeneca R&D Charnwood
Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
H. Lundbeck
Synthesis and pharmacological evaluation of potent and highly selective D3 receptor ligands: inhibition of cocaine-seeking behavior and the role of dopamine D3/D2 receptors.
Universit£
Synthesis and biological characterization of L-N(6)-(1-iminoethyl)lysine 5-tetrazole-amide, a prodrug of a selective iNOS inhibitor.
Pfizer
Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.
The R. W. Johnson Pharmaceutical Research Institute
Synthesis and evaluation of peptidomimetics as selective inhibitors and active site probes of nitric oxide synthases.
Northwestern University
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
Synaptic Pharmaceutical
N(omega)-Nitroarginine-containing dipeptide amides. Potent and highly selective inhibitors of neuronal nitric oxide synthase.
Northwestern University
2-Iminohomopiperidinium salts as selective inhibitors of inducible nitric oxide synthase (iNOS).
Pfizer
2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.
Pfizer
N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity.
Glaxo Wellcome Research and Development
Selective inhibition of neuronal nitric oxide synthase by N omega-nitroarginine-and phenylalanine-containing dipeptides and dipeptide esters.
Northwestern University
Substituted N-phenylisothioureas: potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity.
Glaxo Wellcome Research and Development
Substituted hexahydrobenzo[f]thieno[c]quinolines as dopamine D1-selective agonists: synthesis and biological evaluation in vitro and in vivo.
Abbott Laboratories
2-Iminopiperidine and other 2-iminoazaheterocycles as potent inhibitors of human nitric oxide synthase isoforms.
G. D. Searle Research and Development
3-[[(Aryloxy)alkyl]piperidinyl]-1,2-benzisoxazoles as D2/5-HT2 antagonists with potential atypical antipsychotic activity: antipsychotic profile of iloperidone (HP 873).
Hoechst-Roussel Pharmaceuticals
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Smithkline Beecham Pharmaceuticals
(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).
Abbott Laboratories
The serotonin 5-HT4 receptor. 1. Design of a new class of agonists and receptor map of the agonist recognition site.
Sandoz Pharma
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
Synaptic Pharmaceutical
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Pfizer
Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.
Schering
Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien.
Abbott Laboratories
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.
Glaxo Wellcome Research and Development
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.
Merck Research Laboratories
Design and synthesis of novel dihydropyridine alpha-1a antagonists.
Synaptic Pharmaceutical
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Merck
3,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors.
Neuraxon
Discovery of cis-N-(1-(4-(methylamino)cyclohexyl)indolin-6-yl)thiophene-2-carboximidamide: a 1,6-disubstituted indoline derivative as a highly selective inhibitor of human neuronal nitric oxide synthase (nNOS) without any cardiovascular liabilities.
Neuraxon
Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors.
Neuraxon
Design, synthesis and in vitro evaluation of bridgehead fluoromethyl analogs of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) for the 5-HT(1A) receptor.
Vu University Medical Center
Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitors.
Kalypsys
1,6-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors.
Neuraxon
1,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors.
Neuraxon
Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.
Soochow University College of Pharmaceutical Sciences
Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNO
Kalypsys
Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; the identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor.
Glaxosmithkline
Design, synthesis, radiolabeling, and in vitro and in vivo evaluation of bridgehead iodinated analogues of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635) as potential SPECT ligands for the 5-HT1A receptor.
Vu University Medical Center
Symmetric double-headed aminopyridines, a novel strategy for potent and membrane-permeable inhibitors of neuronal nitric oxide synthase.
Northwestern University
Peripheral but crucial: a hydrophobic pocket (Tyr(706), Leu(337), and Met(336)) for potent and selective inhibition of neuronal nitric oxide synthase.
Northwestern University
Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity fora(1)-adrenoceptors.
University of Copenhagen
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography.
National Institute of Mental Health
Novel N-methylated 8-oxoisoguanines from Pacific sponges with diverse neuroactivities.
Hokkaido University
Potent and selective neuronal nitric oxide synthase inhibitors with improved cellular permeability.
Northwestern University
Fluorinated indazoles as novel selective inhibitors of nitric oxide synthase (NOS): synthesis and biological evaluation.
Uned
L337H mutant of rat neuronal nitric oxide synthase resembles human neuronal nitric oxide synthase toward inhibitors.
Northwestern University
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
European Research Centre For Drug Discovery and Development (Natsyndrugs)
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Pfizer
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.
Pfizer
Design and synthesis of 2-amino-4-methylpyridine analogues as inhibitors for inducible nitric oxide synthase and in vivo evaluation of [18F]6-(2-fluoropropyl)-4-methyl-pyridin-2-amine as a potential PET tracer for inducible nitric oxide synthase.
Washington University
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.
Vanderbilt University
Design, synthesis, and evaluation of potential inhibitors of nitric oxide synthase.
Instituto De QuíMica MéDica
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.
Pharmaceutical Research Institute
Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
(Phenylpiperidinyl)cyclohexylsulfonamides: development of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
(Arylpiperazinyl)cyclohexylsufonamides: discovery of alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of Benign Prostatic Hyperplasia/Lower Urinary Tract Symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
Johnson & Johnson Pharmaceutical Research and Development
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.
Dipartimento Di Scienze Farmaceutiche
Discovery and Optimization of Pyrrolopyrimidine Derivatives as Selective Disruptors of the Perinucleolar Compartment, a Marker of Tumor Progression toward Metastasis.
University of Kansas
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Predix Pharmaceuticals
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
Chungbuk National University
Structural analysis of isoform-specific inhibitors targeting the tetrahydrobiopterin binding site of human nitric oxide synthases.
Sanofi-Aventis
Evaluation of 3-substituted arginine analogs as selective inhibitors of human nitric oxide synthase isozymes.
Nagoya City University
Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.
Lundbeck Research Usa
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
H. Lundbeck
2-Aminopyridines with a shortened amino sidechain as potent, selective, and highly permeable human neuronal nitric oxide synthase inhibitors.
Northwestern University
Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.
Merck Research Laboratories
Nanomolar inhibitors of CNS epinephrine biosynthesis: (R)-(+)-3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines as potent and highly selective inhibitors of phenylethanolamine N-methyltransferase1.
University of Kansas
Novel and orally bioavailable inducible nitric oxide synthase inhibitors: synthesis and evaluation of optically active 4,5-dialkyl-2-iminoselenazolidine derivatives.
Dainippon Pharmaceutical
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.
Merck Research Laboratories
2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution.
Astrazeneca R&D Charnwood
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Virginia Commonwealth University
Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.
Pfizer
Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.
University Hospital Hradec Kralove
Synthesis, bioevaluation and docking studies of new imidamide derivatives as nitric oxide synthase inhibitors.
Universidad De Granada
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.
Southern Medical University
3-Hydroxy-4-methyl-5-pentyl-2-iminopyrrolidine: a potent and highly selective inducible nitric oxide synthase inhibitor.
Pharmacia
Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.
Johnson & Johnson Pharmaceutical Research and Development
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.
Johnson & Johnson Pharmaceutical Research and Development
Structural requirements for inhibition of the neuronal nitric oxide synthase (NOS-I): 3D-QSAR analysis of 4-oxo- and 4-amino-pteridine-based inhibitors.
Aventis Pharma
trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
Università
Selective heterocyclic amidine inhibitors of human inducible nitric oxide synthase.
Pharmacia
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.
Istituto Chimico Farmaceutico E Tossicologico
Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.
University "G. D'Annunzio" of Chieti-Pescara
Determination of the relative and absolute stereochemistry of a potent and alpha1A-selective adrenoceptor antagonist.
Synaptic Pharmaceutical
Novel heterocycles as selective alpha1-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.
Merck Research Laboratories
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
Synaptic Pharmaceutical
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.
Merck
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.
Merck Research Laboratories
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective alpha(1)(a)-adrenergic receptor antagonists.
The R. W. Johnson Pharmaceutical Research Institute
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Abbott Laboratories
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
The R. W. Johnson Pharmaceutical Research Institute
alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor.
The R. W. Johnson Pharmaceutical Research Institute
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.
Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.
Synaptic Pharmaceutical
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Optimization of Blood-Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2-Aminopyridine Scaffold.
Northwestern University
A new class of selective and potent inhibitors of neuronal nitric oxide synthase.
Pfizer
Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.
Warner-Lambert
N-Substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as D(2) antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents.
Knoll Pharmaceuticals
Synthesis and evaluation of new sulfur-containing L-arginine-derived inhibitors of nitric oxide synthase.
Wake Forest University
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.
Merck
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.
University of Florida
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).
Centro De InvestigacióN Grupo Ferrer
Synthesis of boronic acid analogs of L-arginine as alternate substrates or inhibitors of nitric oxide synthase.
Université
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
Merck
Isoindolinone enantiomers having affinity for the dopamine D4 receptor.
Parke-Davis Pharmaceutical Research
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate.
Northwestern University
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
Merck
Acetamidine lysine derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide dihydrochloride: a highly selective inhibitor of human inducible nitric oxide synthase.
Searle
Substituted 2-iminopiperidines as inhibitors of human nitric oxide synthase isoforms.
G. D. Searle Research and Development
Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign pr
Abbott Laboratories
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.
Warner-Lambert
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as ?1A/1D-AR subselective antagonists for BPH.
Jinan University
Phenyl Ether- and Aniline-Containing 2-Aminoquinolines as Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase.
Northwestern University
Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.
Solvay Duphar
6-methoxy-7-benzofuranoxy and 6-methoxy-7-indolyloxy analogues of 2-[2-(2,6-Dimethoxyphenoxy)ethyl]aminomethyl-1,4-benzodioxane (WB4101):1 discovery of a potent and selective ?1D-adrenoceptor antagonist.
Universit£
Synthesis and biological evaluation of 4,5-dihydro-1H-pyrazole derivatives as potential nNOS/iNOS selective inhibitors. Part 2: Influence of diverse substituents in both the phenyl moiety and the acyl group.
Universidad De Granada
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Smithkline Beecham Pharmaceuticals
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists.
Drug Discovery Laboratory
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
Universit£
Structure-activity relationships in 1,4-benzodioxan-related compounds. 8.(1) {2-[2-(4-chlorobenzyloxy)phenoxy]ethyl}-[2-(2,6-dimethoxyphenoxy)ethyl]amine (clopenphendioxan) as a tool to highlight the involvement of alpha1D- and alpha1B-adrenoreceptor subtypes in the regulation of human PC-3 prostate
Universit£
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.
University of Bologna
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Glaxosmithkline Research Laboratories
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.
University of Bologna
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.
University of Camerino
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
New York University Medical Center
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
University of Camerino
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Synthesis, biological evaluation and SAR of naftopidil-based arylpiperazine derivatives.
Luoyang Normal University
Identification of 3,4-dihydro-2H-thiochromene 1,1-dioxide derivatives with a phenoxyethylamine group as highly potent and selective ?
Takeda Pharmaceutical
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Novel naftopidil derivatives containing methyl phenylacetate and their blocking effects on ?
Guangzhou Medical University
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Nitrile in the Hole: Discovery of a Small Auxiliary Pocket in Neuronal Nitric Oxide Synthase Leading to the Development of Potent and Selective 2-Aminoquinoline Inhibitors.
Northwestern University
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D
Universit£
The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT
Universit£
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.
Northwestern University
Improvement of Cell Permeability of Human Neuronal Nitric Oxide Synthase Inhibitors Using Potent and Selective 2-Aminopyridine-Based Scaffolds with a Fluorobenzene Linker.
Northwestern University
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na
Department of Discovery Chemistry Merck
Developing dual and specific inhibitors of dimethylarginine dimethylaminohydrolase-1 and nitric oxide synthase: toward a targeted polypharmacology to control nitric oxide.
The University of Texas
Role of zinc in isoform-selective inhibitor binding to neuronal nitric oxide synthase .
University of California Irvine
Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.
Case Western Reserve University
(Phenylpiperazinyl)cyclohexylureas: discovery of alpha1a/1d-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).
Johnson & Johnson Pharmaceutical Research and Development
Differential effects of the 5-hydroxytryptamine (5-HT)1A receptor inverse agonists Rec 27/0224 and Rec 27/0074 on electrophysiological responses to 5-HT1A receptor activation in rat dorsal raphe nucleus and hippocampus in vitro.
Universit&Aagrove
Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.
Kyowa Hakko Kogyo
S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.
Institut De Recherches Servier
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.
Institut De Recherches Servier
Biochemistry and pharmacology of epitope-tagged alpha(1)-adrenergic receptor subtypes.
Emory University
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.
Abbott Laboratories
N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-nitrophenyl) cyclohexanecarboxamide: a novel pre- and postsynaptic 5-hydroxytryptamine(1A) receptor antagonist active on the lower urinary tract.
Recordati
OPC-28326, a selective femoral vasodilator, is an alpha2C-adrenoceptor-selective antagonist.
Otsuka Maryland Research Institute
Rabbit alpha2-adrenoceptors: both platelets and adipocytes have alpha2A-pharmacology.
Glaxosmithkline
Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization.
Institut De Recherches Servier
S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine.
Centre De Recherches De Croissy
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626.
Centre De Recherches De Croissy
Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states.
Institut De Recherches Servier
SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist.
Smithkline Beecham Pharmaceuticals
Pharmacological characterization of two novel and potent 5-HT4 receptor agonists, RS 67333 and RS 67506, in vitro and in vivo.
Syntex Discovery Research
Species orthologs of the alpha-2A adrenergic receptor: the pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors.
University of Nebraska
The pharmacological profile of cloned and stably expressed alpha 1b-adrenoceptor in CHO cells.
National Children'S Medical Research Center
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
The Scripps Research Institute
Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models.
Kalypsys