PMID

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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

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

Combined Interactions with I

University of Camerino

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?

University of Camerino

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.

University of Camerino

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

2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A

National Institute of Diabetes and Digestive and Kidney Disease

Catecholamine Derivatives: Natural Occurrence, Structural Diversity, and Biological Activity.

Shandong University

Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist.

Università

BAY-6096: A Potent, Selective, and Highly Water-Soluble Adrenergic α

Bayer

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

Discovery and

Small Pharma.

A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research.

Xiamen University

Targeting σ

The University of Texas At Austin

Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.

High Point University

Design and Synthesis of Orally Active Quinolyl Pyrazinamides as Sigma 2 Receptor Ligands for the Treatment of Pancreatic Cancer.

University of Michigan

Discovery of 2-Aminopyrimidines as Potent Agonists for the Bitter Taste Receptor TAS2R14.

Friedrich-Alexander-Universitat Erlangen-Nurnberg

Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.

Juvantia Pharma

Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y

National Institute of Diabetes and Digestive and Kidney Diseases

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

The Essential Medicinal Chemistry of Cannabidiol (CBD).

University of Minnesota

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

Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1

Division of Janssen-Cilag

3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT

University of Minnesota Twin Cities

Fluorinated analogues of marsanidine, a highly α2-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.

University of Camerino

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

Return of D

University of Nebraska Medical Center

Discovery of selective, orally bioavailable, N-linked arylsulfonamide Na

Department of Discovery Chemistry Merck

Psychedelics and the human receptorome.

University of Oklahoma

Pyrazolopyrimidine compounds as adenosine receptor antagonists

Exscientia

(Thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists

Eli Lilly

WAY-100635 is a potent dopamine D4 receptor agonist.

Purdue University

Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.

Mcgill University

SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.

Sanofi-Synthelabo Recherche

S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: I. Cellular, electrophysiological, and neurochemical profile in comparison with ropinirole.

Institut De Recherches Servier

In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates.

National Institute On Drug Abuse

Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology.

Case Western Reserve University

3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro.

Case Western Reserve University

L-homocysteine sulfinic acid and other acidic homocysteine derivatives are potent and selective metabotropic glutamate receptor agonists.

Case Western Reserve University

H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs.

Case Western Reserve University

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

In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs.

WestfÄLische Wilhelms-UniversitÄ

Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.

Novartis Pharma

The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.

Case Western Reserve University

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Janssen Research Foundation

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

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

Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding.

Roche Bioscience

Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.

Janssen Research Foundation

The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.

University of Michigan

Cloning, expression, and pharmacological characterization of a human alpha 2B-adrenergic receptor.

Neurogenetic

Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.

University of Nebraska