Discovery of an Orally Bioavailable NK1 Receptor Antagonist, (2S,3S)-(2-Methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with Potent Antiemetic Activity

Journal of Medicinal Chemistry

Volumn 38, Issue 26, 1995, Pages 4985-4992

  Ward, Peter ^a   Armour, Duncan R ^a   Bays, David E ^a   Evans, Brian ^a   Giblin, Gerard M P ^a   Heron, Nicola ^a   Hubbard, Tania ^a   Liang, Kai ^a   Middlemiss, David ^a   Mordaunt, Jackie ^a   Naylor, Alan ^a   Pegg, Neil A ^a   Vinader, M Victoria ^a   Watson, Stephen P ^a   Bountra, Chas ^a   Evans, David C ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 BENZHYDRYL 3 (2 METHOXYBENZYLAMINO) 1 AZABICYCLO[2.2.2]OCTANE; 3 (2 METHOXYBENZYLAMINO) 2 PHENYLPIPERIDINE; [2 METHOXY 5 (1 TETRAZOLYL)BENZYL](2 PHENYL 3 PIPERIDINYL)AMINE; ANTIEMETIC AGENT; TACHYKININ RECEPTOR ANTAGONIST;

ARTICLE; CANCER CHEMOTHERAPY; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG POTENCY; DRUG STABILITY; LIPOPHILICITY; NONHUMAN; VOMITING;

ANIMALS; ANTIEMETICS; BIOLOGICAL AVAILABILITY; CELL MEMBRANE; CHO CELLS; CRICETINAE; DOGS; FEMALE; FERRETS; GERBILLINAE; MAGNETIC RESONANCE SPECTROSCOPY; MALE; PIPERIDINES; RECEPTORS, NEUROKININ-1; TACHYKININS; TETRAZOLES; VOMITING; WHOLE-BODY IRRADIATION;

EID: 0029585287     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm00026a005     Document Type: Article

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