Functional and pharmacological characterization of the first specific agonist and antagonist for the V1b receptor in mammals
Details
Serval ID
serval:BIB_53A10873779D
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Institution
Title
Functional and pharmacological characterization of the first specific agonist and antagonist for the V1b receptor in mammals
Journal
Stress
ISSN
1025-3890 (Print)
Publication state
Published
Issued date
09/2003
Volume
6
Number
3
Pages
199-206
Notes
Journal Article
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.
Review --- Old month value: Sep
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, P.H.S.
Review --- Old month value: Sep
Abstract
By activating three distinct vasopressin receptor isoforms called V1a-R, V1b-R (V3-R) and V2-R, vasopressin (VP) mediates a wide number of biological effects in mammals and may be involved in several pathological states. Up to now only specific V1a and V2 receptor agonists and antagonists have been successfully designed. The role of the V1b-R still remains partially unknown, due to the lack of selective V1b-R ligands and orally-active molecules, which are crucial tools for investigating the central and peripheral functions or pathological disorders associated with this receptor. In this review, we report the biological and pharmacological properties of the first two specific V1b-R ligands: d[Cha4] AVP, a high affinity V1b-R agonist and SSR149415, a potent orally-active V1b-R antagonist with good selectivity with respect to other VP/OT receptor isoforms and able to control ACTH secretion in vitro and in vivo. Indeed, these molecules constitute invaluable tools for exploring the central and peripheral roles of VP mediated via V1b receptors. Interestingly, SSR149415 displays potent anxiolytic and antidepressant-like activities, indicating that this new class of drugs has a promising therapeutical potential in the treatment of stress-related disorders, anxiety and depression.
Keywords
Animals
Arginine Vasopressin/*analogs & derivatives/*pharmacology
Humans
Indoles/*pharmacology
Pyrrolidines/*pharmacology
Receptors, Vasopressin/*agonists/*antagonists & inhibitors
Pubmed
Web of science
Create date
15/02/2008 16:57
Last modification date
20/08/2019 14:08