Full biological characterization of two linear vasopressin analogues - [Phaa,D-Tyr(Et).sup.2./sup.,Aib.sup.4./sup.,Arg.sup.6./sup.,Tyr(NH.sub.2./sub.).sup.9./sup.]AVP and [Phaa,D-Tyr(Et).sup.2./sup.,Arg.sup.6./sup.,Aib.sup.7./sup.,Tyr(NH.sub.2./sub.).sup.9./sup.]AVP

0193680 - UOCHB-X 20000030 RIV SIGLE CZ eng C - Conference Paper (international conference)
Kunčarová, Pavla - Nazarov, Elšan - Howl, J. - Slaninová, Jiřina
Full biological characterization of two linear vasopressin analogues - [Phaa,D-Tyr(Et)²,Aib⁴,Arg⁶,Tyr(NH₂)⁹]AVP and [Phaa,D-Tyr(Et)²,Arg⁶,Aib⁷,Tyr(NH₂)⁹]AVP.
80-86241-06-8. In: Biologically Active Peptides. Praha: ÚOCHB AVČR, 1999 - (Slaninová, J.; Barth, T.), s. 41-43. Collection Symposium Series., 3.
[Biologically Active Peptides. Conference /6./. Praha (CZ), 21.04.1999-23.04.1999]
R&D Projects: GA AV ČR KSK2055603
Institutional research plan: CEZ:AV0Z4055905
Keywords : Biological activity * Vasopressin antagonists
Subject RIV: CE - Biochemistry

The achiral amino acid Aib was introduced into position 4 or 7 of the linear V1a-selective vasopressin antagonist [Phaa,D-Tyr(Et)2,Arg6,Tyr(NH2)9]AVP. Peptides displayed reduced affinities for both V1a and V2 receptors and high antipressor activity in vivo. Uterotonic tests in vitro revealed that these compounds also strongly interact with the oxytocin receptor (pA2=7.8 and 7.9 for Aib4 and Aib7, respectively).
Permanent Link: http://hdl.handle.net/11104/0089375