PMID

Data

Article Title

Organization

Flavones. 2. Synthesis and structure-activity relationship of flavodilol and its analogues, a novel class of antihypertensive agents with catecholamine depleting properties.

Pennwalt

Carbostyril derivatives having potent beta-adrenergic agonist properties.

TBA

Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism.

TBA

Affinity labels for beta-adrenoceptors: preparation and properties of alkylating beta-blockers derived from indole.

TBA

Alkylating beta-blockers: activity of isomeric bromoacetyl alprenolol menthanes.

TBA

Syntheses and adrenergic agonist properties of ring-fluorinated isoproterenols.

TBA

Synthesis and adrenoceptor affinity of some highly polar beta-substituted catecholamines.

TBA

beta-Adrenergic blocking agents. alpha- and gamma-methyl(aryloxy)propanolamines.

TBA

Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines.

TBA

Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.

Merck Research Laboratories

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 novel N-phenylglycine derivatives as potent and selective beta(3)-adrenoceptor agonists for the treatment of frequent urination and urinary incontinence.

Kissei Pharmaceutical

Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.

TBA

Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.

Smithkline Beecham Pharmaceuticals

Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.

National Institute of Diabetes and Digestive and Kidney Diseases

SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.

Searle Research and Development

Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.

Bristol-Myers Squibb

Design and synthesis of propranolol analogues as serotonergic agents.

Virginia Commonwealth University

Syntheses and adrenergic activities of ring-fluorinated epinephrines.

National Institute of Diabetes

Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans.

TBA

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

 

SYNTHESIS AND BIOLOGICAL EVALUATION OF A FLUORINATED ANALOG OF THE β-ADRENERGIC BLOCKING AGENT, METOPROLOL

TBA

 

Asymmetric synthesis of FR165914: A novel β₃-adrenergic agonist with a benzocycloheptene structure

TBA

Potent oxindole based human beta3 adrenergic receptor agonists.

Eli Lilly

Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

Pfizer

Potent benzimidazolone based human beta(3)-adrenergic receptor agonists.

Eli Lilly

(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors.

Wyeth Research (Uk)

Chemistry, binding affinities, and behavioral properties of a new class of"antineophobic" mitochondrial DBI receptor complex (mDRC) ligands.

Mayo Foundation

3,4-Dimethyl-4-(3-hydroxyphenyl)piperidines: opioid antagonists with potent anorectant activity.

Eli Lilly

Nondepressant beta-adrenergic blocking agents. 1. Substituted 3-amino-1-(5,6,7,8-tetrahydro-1-naphthoxy)-2-propanols.

TBA

Synthesis and biological properties of 2-, 5-, and 6-fluoronorepinephrines.

TBA

Development of high-affinity 5-HT3 receptor antagonists. Structure-affinity relationships of novel 1,7-annelated indole derivatives.

Solvay Duphar

A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.

Monash University

In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.

TBA

Effect of fluorine substitution on the adrenergic properties of 3-(tert-butylamino)-1-(3,4-dihydroxyphenoxy)-2-propanol.

National Institute of Diabetes

Analogues of the 5-HT1A serotonin antagonist 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl]piperazine with reduced alpha 1-adrenergic affinity.

Virginia Commonwealth University

Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent.

American Cyanamid