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 - Konferenční příspěvek (zahraniční konf.)
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]
Grant CEP: GA AV ČR KSK2055603
Výzkumný záměr: CEZ:AV0Z4055905
Klíčová slova: Biological activity * Vasopressin antagonists
Kód oboru RIV: CE - Biochemie

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).
Trvalý link: http://hdl.handle.net/11104/0089375