118 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
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
The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The"Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Virginia Commonwealth University
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples.
University of Kansas
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.
University of Illinois At Chicago
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.
The Alexander Shulgin Research Institute
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.
City University of New York
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.
City University of New York
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
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Merck Research Laboratories
Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.
University of Illinois At Chicago
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Novartis Pharma
Absolute configuration of glycerol derivatives. 7. Enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzodioxane (WB-4101), a potent competitive alpha-adrenergic antagonist.
TBA
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
TBA
Favourable involvement ofa2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement.
University of Camerino
Might the observeda(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?
Universit£
Fruitful adrenergica(2C)-agonism/a(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
Universita` Di Camerino
Rigid analogues of thea2-adrenergic blocker atipamezole: small changes, big consequences.
Pierre Fabre Research Center
Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?
Universita Degli Studi Di Camerino
Alpha2-adrenoreceptors profile modulation. 4. From antagonist to agonist behavior.
Universit£
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha 2-antagonistic activity as potential antidepressants.
Janssen Research Foundation
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
Methylation of imidazoline related compounds leads to loss ofa2-adrenoceptor affinity. Synthesis and biological evaluation of selective I1 imidazoline receptor ligands.
University of Strasburg
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands.
The University of Sydney
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
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
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.
Kyowa Hakko Kogyo
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Janssen-Cilag
trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new dopamine D1 receptor full agonist.
Purdue University
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Novartis Institutes For Biomedical Research
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
National Taiwan University
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Smithkline Beecham Pharmaceuticals
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
Synaptic Pharmaceutical
Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.
University of Tennessee
Design and synthesis of novel dihydropyridine alpha-1a antagonists.
Synaptic Pharmaceutical
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands.
The University of Sydney
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
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
Facile synthesis of octahydrobenzo[h]isoquinolines: novel and highly potent D1 dopamine agonists.
Purdue University
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).
Siena Biotech
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways.
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj
(-)-Dibromophakellin: an alpha2B adrenoceptor agonist isolated from the Australian marine sponge, Acanthella costata.
Griffith University
Identification and SAR around N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist.
Pfizer
Synthesis and evaluation of [N-methyl-11C]N-desmethyl-loperamide as a new and improved PET radiotracer for imaging P-gp function.
National Institute of Mental Health
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Merck Research Laboratories
Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.
Università
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography.
National Institute of Mental Health
Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
Juvantia Pharma
Evaluation of the eutomer of 4-{3-(4-chlorophenyl)-3-hydroxypyrrolidin-1-yl}-1-(4-fluorophenyl)butan-1-one, {(+)-SYA 09}, a pyrrolidine analog of haloperidol.
Florida A&M University
1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
Alcon Research
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
Bioisosteric phentolamine analogs as potent alpha-adrenergic antagonists.
Chungbuk National University
Synthesis and biological studies of yohimbine derivatives on human alpha2C-adrenergic receptors.
University of Tennessee
Distal kinetic deuterium isotope effect: Phenyl ring deuteration attenuates N-demethylation of Lu AF35700.
H. Lundbeck
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Janssen-Cilag
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
Binding of beta-carbolines at 5-HT(2) serotonin receptors.
Virginia Commonwealth University
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha(2)-adrenoceptor antagonistic activities: a novel series of potential antidepressants.
Johnson & Johnson Pharmaceutical Research & Development
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Universita Di Camerino
Exploration of Alternative Scaffolds for P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge
University of Mississippi
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
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
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D
National Institute of Neurological Disorders and Stroke
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D
University of Pennsylvania
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
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.
Synaptic Pharmaceutical
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT
University of Minnesota Twin Cities
Fluorinated analogues of marsanidine, a highly ?2-AR/imidazoline I1 binding site-selective hypotensive agent. Synthesis and biological activities.
Medical University of Gdansk
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
University of Camerino
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
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
Qbi Covid-19 Research Group (Qcrg)
alpha 2-adrenoreceptors profile modulation. 2. Biphenyline analogues as tools for selective activation of the alpha 2C-subtype.
Universit£
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Glaxosmithkline Research Laboratories
2-amino-2-oxazolines as subtype selective alpha(2) adrenoceptor agonists.
Lundbeck Research Usa
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
Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Texas Tech University Health Sciences Center
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.
University of Texas At Austin
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na
Department of Discovery Chemistry Merck
