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Titolo:
Pharmacological profile of T-1032, a novel specific phosphodiesterase type5 inhibitor, in isolated rat aorta and rabbit corpus cavernosum
Autore:
Takagi, M; Mochida, H; Noto, T; Yano, K; Inoue, H; Ikeo, T; Kikkawa, K;
Indirizzi:
Tanabe Seiyaku Co Ltd, Discovery Res Lab, Toda, Saitama 3358505, Japan Tanabe Seiyaku Co Ltd Toda Saitama Japan 3358505 , Saitama 3358505, Japan
Titolo Testata:
EUROPEAN JOURNAL OF PHARMACOLOGY
fascicolo: 1-2, volume: 411, anno: 2001,
pagine: 161 - 168
SICI:
0014-2999(20010105)411:1-2<161:PPOTAN>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES; NITRIC-OXIDE; GUANYLYL CYCLASE; SMOOTH-MUSCLE; ERECTILE DYSFUNCTION; IN-VITRO; SILDENAFIL; RELAXATION; CGMP; NITROPRUSSIDE;
Keywords:
phosphodiesterase type 5 inhibitor; aorta, rat; corpus cavernosum, rabbit; relaxation; cyclic nucleotide;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
42
Recensione:
Indirizzi per estratti:
Indirizzo: Kikkawa, K Tanabe Seiyaku Co Ltd, Discovery Res Lab, 2-2-50 Kawagishi, Toda, Saitama 3358505, Japan Tanabe Seiyaku Co Ltd 2-2-50 Kawagishi Toda Saitama Japan 3358505
Citazione:
M. Takagi et al., "Pharmacological profile of T-1032, a novel specific phosphodiesterase type5 inhibitor, in isolated rat aorta and rabbit corpus cavernosum", EUR J PHARM, 411(1-2), 2001, pp. 161-168

Abstract

This study was designed to examine the pharmacological properties of T-1032 (methyl-2-(4-aminophenyl)-1,2-dihydro-1-oxo-7-(2-pysidinylmethoxy)-4-(3,4,5-trimethoxyphenyl)-3-isoquinoline carboxy late sulfate), a novel phosphodiesterase type 5 inhibitor, in isolated rat aorta and rabbit corpus cavernosum. T-1032 (3 x 10(-11) to 3 x 10(-7) M) caused an endothelium-dependent relaxation in the isolated rat aorta precontracted with phenylephrine. and the relaxation was accompanied by an increase in cGMP but not cAMP levels. The T-1032-induced relaxation was attenuated by NG-nitro-L-arginine methyl ester (L-NAME) (10(-3) M), a nitric oxide (NO) synthase inhibitor. or 1H-[1,2.4]oxadiazolo[4,3-alpha ]quinoxalin-1-one (ODQ) (10(-5) M), a guanylyl cyclase inhibitor. T-1032 (10(-9), 10(-8) M) produced a potentiation of the relaxation induced by sodium nitroprusside, but not of the relaxation inducedby isoproterenol. In the isolated rabbit corpus cavernosum precontracted with phenylephrine. the electrical field stimulation-induced relaxation was attenuated by treatment with tetrodotoxin(10(-6) M) as well as L-NAME(10(-4) M). The L-NAME-inhibited relaxation was restored by treatment with L-arginine (5 x 10(-4) M). T-1032 (10(-9) to 10(-6) M) and sildenafil (10(-9) to 10(-6) M) produced a potentiation of the electrical field stimulation-induced relaxation as well as a decrease in basal tension in a concentration-dependent manner. It was concluded that T-1032 had potentiating effects on theNO/cGMP signaling pathway in isolated tissues. probably through specific blockade of phosphodiesterase type 5. T-1032 would be a useful compound to examine the physiologic functions of phosphodiesterase type 5 in mammalian tissues. (C) 2001 Elsevier Science B.V. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/04/20 alle ore 11:21:10