Establishment and validation of a rabbit model for in vivo pharmacodynamic screening of tachykinin NK2 antagonists

Journal of Pharmacological Sciences

Volumn 118, Issue 4, 2012, Pages 487-495

  Tanaka, Takahiro ^a   Matsumoto Okano, Shiho ^a   Inatomi, Nobuhiro ^a   Fujioka, Yasushi ^a   Kamiguchi, Hidenori ^a   Yamaguchi, Masashi ^a   Imanishi, Akio ^a   Kawamoto, Makiko ^a   Miura, Kasei ^a   Nishikawa, Yoichi ^a   Tsukimi, Yasuhiro ^a  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

Author keywords

Colonic contraction; Colorectal distension; Pharmacodynamic (PD) marker; Pharmacokinetic (PK) pharmacodynamic (PD)

Indexed keywords

1 PHENYL 3 [2 [(4 PHENYL 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL)CARBONYL]CYCLOHEXYL]UREA; 1 [4 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]TETRAHYDRO 2H PYRAN 3 YL] 3 [4 (3 METHYL 1H PYRAZOL 1 YL)PHENYL]UREA; 1 [4 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]TETRAHYDRO 2H PYRAN 3 YL] 3 [6 (1H PYRAZOL 1 YL)PYRIDIN 3 YL]UREA; 1 [4 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]TETRAHYDRO 2H PYRAN 3 YL] 3 [6 (3 METHYL 1H PYRAZOL 1 YL)UREA]; 1 [4,4 DIFLUORO 2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL] 3 (4 METHOXYPHENYL)UREA; 4 (DIFLUOROMETHOXY) N [2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL]BENZAMIDE; 4 (N HYDROXYETHANIMIDOYL) N [2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL]BENZAMIDE; 4 CHLORO N [4,4 DIFLUORO 2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL]BENZAMIDE; ANALGESIC AGENT; BETA ALANINE 8 NEUROKININ A[4-10]; N [2 [(4 PHENYL 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL)CARBONYL]CYCLOHEXYL]BENZAMIDE; N [4 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL] 1 METHYLPIPERIDIN 3 YL] 4 (3 METHYL 1 1H PYRAZOL 1 YL)BENZAMIDE; N [4,4 DIFLUORO 2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL] 4 (3 METHYL 1H PYRAZOL 1 YL)BENZAMIDE; N [4,4 DIFLUORO 2 [[4 (METHOXYMETHYL) 2,3,3A,4,5,9B HEXAHYDRO 1H PYRROL[3,2 C]QUINOLIN 1 YL]CARBONYL]CYCLOHEXYL] 4 METHOXYBENZAMIDE; NEUROKININ 2 RECEPTOR AGONIST; NEUROKININ 2 RECEPTOR ANTAGONIST; OPIATE ANTAGONIST; SAREDUTANT; UNCLASSIFIED DRUG;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING SITE; COLON DISEASE; COLORECTAL DISEASE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BINDING; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG POTENCY; DRUG RESPONSE; DRUG SCREENING; HIGH THROUGHPUT SCREENING; HYPERSENSITIVITY; IC 50; IN VITRO STUDY; IN VIVO STUDY; INTESTINE CONTRACTION; IRRITABLE COLON; NONHUMAN; RABBIT;

EID: 84866560749     PISSN: 13478613     EISSN: 13478648     Source Type: Journal    
DOI: 10.1254/jphs.11245FP     Document Type: Article

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