Literature DB >> 1850553

OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist.

Y Yamamura1, H Ogawa, T Chihara, K Kondo, T Onogawa, S Nakamura, T Mori, M Tominaga, Y Yabuuchi.   

Abstract

An orally effective, nonpeptide, vasopressin V1 receptor antagonist, OPC-21268, has been identified. This compound selectively antagonized binding to the V1 subtype of the vasopressin receptor in a competitive manner. In vivo, the compound acted as a specific antagonist of arginine vasopressin (AVP)-induced vasoconstriction. After oral administration in conscious rats, the compound also antagonized pressor responses to AVP. OPC-21268 can be used to study the physiological role of AVP and may be therapeutically useful in the treatment of hypertension and congestive heart failure.

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Year:  1991        PMID： 1850553     DOI： 10.1126/science.1850553

Source DB:  PubMed          Journal:  Science        ISSN： 0036-8075            Impact factor:   47.728


  30 in total

1.  Pharmacologic characterization of the oxytocin receptor in human uterine smooth muscle cells.

Authors:  A Tahara; J Tsukada; Y Tomura; K i Wada; T Kusayama; N Ishii; T Yatsu; W Uchida; A Tanaka
Journal:  Br J Pharmacol       Date:  2000-01       Impact factor: 8.739

2.  Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes.

Authors:  S Nakamura; Y Yamamura; S Itoh; T Hirano; K Tsujimae; M Aoyama; K Kondo; H Ogawa; T Shinohara; K Kan; Y Tanada; S Teramoto; T Sumida; S Nakayama; K Sekiguchi; T Kambe; G Tsujimoto; T Mori; M Tominaga
Journal:  Br J Pharmacol       Date:  2000-04       Impact factor: 8.739

3.  Effects of YM471, a nonpeptide AVP V(1A) and V(2) receptor antagonist, on human AVP receptor subtypes expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells.

Authors:  J Tsukada; A Tahara; Y Tomura; T Kusayama; N Ishii; T Yatsu; W Uchida; N Taniguchi; A Tanaka
Journal:  Br J Pharmacol       Date:  2001-07       Impact factor: 8.739

4.  Molecular modeling of interactions of the non-peptide antagonist YM087 with the human vasopressin V1a, V2 receptors and with oxytocin receptors.

Authors:  A Giełdoń; R Kaźmierkiewicz; R Slusarz; J Ciarkowski
Journal:  J Comput Aided Mol Des       Date:  2001-12       Impact factor: 3.686

Review 5.  The roles of V1a vasopressin receptors in blood pressure homeostasis: a review of studies on V1a receptor knockout mice.

Authors:  Yoko Fujiwara; Akito Tanoue; Gozoh Tsujimoto; Taka-Aki Koshimizu
Journal:  Clin Exp Nephrol       Date:  2011-11-01       Impact factor: 2.801

6.  Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.

Authors:  Cristiana Griffante; Andrew Green; Ornella Curcuruto; Carl P Haslam; Bryony A Dickinson; Roberto Arban
Journal:  Br J Pharmacol       Date:  2005-11       Impact factor: 8.739

7.  The 3D structure of the binding pocket of the human oxytocin receptor for benzoxazine antagonists, determined by molecular docking, scoring functions and 3D-QSAR methods.

Authors:  Balázs Jójárt; Tamás A Martinek; Arpád Márki
Journal:  J Comput Aided Mol Des       Date:  2005-05       Impact factor: 3.686

8.  V1a vasopressin receptors maintain normal blood pressure by regulating circulating blood volume and baroreflex sensitivity.

Authors:  Taka-aki Koshimizu; Yoshihisa Nasa; Akito Tanoue; Ryo Oikawa; Yuji Kawahara; Yasushi Kiyono; Tetsuya Adachi; Toshiki Tanaka; Tomoyuki Kuwaki; Toyoki Mori; Satoshi Takeo; Hitoshi Okamura; Gozoh Tsujimoto
Journal:  Proc Natl Acad Sci U S A       Date:  2006-05-08       Impact factor: 11.205

Review 9.  Impact of high-throughput screening in biomedical research.

Authors:  Ricardo Macarron; Martyn N Banks; Dejan Bojanic; David J Burns; Dragan A Cirovic; Tina Garyantes; Darren V S Green; Robert P Hertzberg; William P Janzen; Jeff W Paslay; Ulrich Schopfer; G Sitta Sittampalam
Journal:  Nat Rev Drug Discov       Date:  2011-03       Impact factor: 84.694

Review 10.  Molecular neurobiology and pharmacology of the vasopressin/oxytocin receptor family.

Authors:  J Peter; H Burbach; R A Adan; S J Lolait; F W van Leeuwen; E Mezey; M Palkovits; C Barberis
Journal:  Cell Mol Neurobiol       Date:  1995-10       Impact factor: 5.046
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