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SB-656104-A: a novel 5-HT(7) receptor antagonist with improved in vivo properties.

Glaxosmithkline

Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.

Glaxosmithkline

Discovery of dual positive allosteric modulators (PAMs) of the metabotropic glutamate 2 receptor and CysLT1 antagonists for treating migraine headache.

Eli Lilly

Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1 F receptor agonists: Evolution from bicyclic to monocyclic cores.

Eli Lilly

Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.

Glaxosmithkline

The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.

Smithkline Beecham Pharmaceuticals

Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).

Smithkline Beecham Pharmaceuticals

Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.

Wyeth Research

N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.

Eli Lilly

Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.

Glaxosmithkline

Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide.

Theravance

Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.

Beijing Normal University

Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists.

Eli Lilly

Design, synthesis and biological evaluation of pyridinylmethylenepiperidine derivatives as potent 5-HT

Sunshine Lake Pharma

Substituted furo[3,2-b]pyridines: novel bioisosteres of 5-HT 1F receptor agonists.

Eli Lilly

Novel potent 5-HT(1F) receptor agonists: structure-activity studies of a series of substituted N-[3-(1-methyl-4-piperidinyl)-1H-pyrrolo[3,2-b]pyridin-5-yl]amides.

Eli Lilly

Identification of a novel series of selective 5-HT7 receptor antagonists.

Glaxosmithkline

N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.

Merck Sharp & Dohme Research Laboratories

Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.

Glaxosmithkline

3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists.

Merck Sharp & Dohme Research Laboratories

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

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.

Merck Sharp And Dohme Research Laboratories

Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.

Glaxosmithkline

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.

Glaxosmithkline

Discovery of 4-[3-(trans-3-dimethylaminocyclobutyl)-1H-indol-5-ylmethyl]-(4S)-oxazolidin-2-one (4991W93), a 5HT(1B/1D) receptor partial agonist and a potent inhibitor of electrically induced plasma extravasation.

Glaxowellcome

Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors.

Northwestern University

Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors.

Eli Lilly

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

Janssen Research Foundation

Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A.

Smithkline Beecham Pharmaceuticals

A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).

Smithkline Beecham Pharmaceuticals

Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.

Smithkline Beecham Pharmaceuticals

SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.

Smithkline Beecham Pharmaceuticals

(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist.

Smithkline Beecham Pharmaceuticals

Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine.

Eli Lilly

SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors.

Smithkline Beecham Pharmaceuticals

BW 723C86, a 5-HT2B receptor agonist, causes hyperphagia and reduced grooming in rats.

Smithkline Beecham Pharmaceuticals

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

Janssen Research Foundation

In vitro and in vivo profile of SB 206553, a potent 5-HT2C/5-HT2B receptor antagonist with anxiolytic-like properties.

Smithkline Beecham Pharmaceuticals

Effects of the 5-HT2B receptor agonist, BW 723C86, on three rat models of anxiety.

Smithkline Beecham Pharmaceuticals

Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase.

Synaptic Pharmaceutical

Molecular biology of 5-HT receptors.

University Of Alberta