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Vasopressin V1b receptor (V1BR) also known as vasopressin 3 receptor (VPR3) or antidiuretic hormone receptor 1B is a protein that in humans is encoded by the AVPR1B (arginine vasopressin receptor 1B) gene. V1BR acts as a receptor for vasopressin. AVPR1B belongs to the subfamily of G protein-coupled receptors.
The human V 3 receptor (V 3 R, previously known as V 1B R) is a G-protein-coupled pituitary receptor that, because of its scarcity, was only recently characterized. [1] The 424-amino-acid sequence of the V 3 R has homologies of 45%, 39%, and 45% with the V 1 R, V 2 R and oxytocin receptor (OTR), respectively.
Vasopressin agonists are used therapeutically in various conditions, and its long-acting synthetic analogue desmopressin is used in conditions featuring low vasopressin secretion, as well as for control of bleeding (in some forms of von Willebrand disease and in mild haemophilia A) and in extreme cases of bedwetting by children.
The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors (V 1A, V 1B and V 2).These receptors have a variety of functions, with the V 1A and V 2 receptors are expressed peripherally and involved in the modulation of blood pressure and kidney function respectively, while the V 1A and V 1B receptors are expressed in the central nervous system.
Brezivaptan [1] (developmental code names ANC-501, THY-1773, TS-121) is an orally active, selective vasopressin V 1B receptor antagonist which is under development by Taisho Pharmaceutical for the adjunctive treatment of major depressive disorder. [2] [3] [4] As of November 2022, it is in phase II clinical trials for this indication. [2] [3] [5]
551 11998 Ensembl ENSG00000101200 ENSMUSG00000037727 UniProt P01185 P35455 RefSeq (mRNA) NM_000490 NM_009732 RefSeq (protein) NP_000481 NP_033862 Location (UCSC) Chr 20: 3.08 – 3.08 Mb Chr 2: 130.42 – 130.42 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Human vasopressin, also called antidiuretic hormone (ADH), arginine vasopressin (AVP) or argipressin, is a hormone synthesized ...
Nelivaptan [1] (developmental codename SSR-149,415) is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V 1B subtype. [2] The drug had entered clinical trials for treatment of anxiety and depression. [3] In July 2008, Sanofi-Aventis announced that further development of this drug had been halted. [4]
ABT-436 is an orally active, highly selective vasopressin V 1B receptor antagonist which was under development by Abbott Laboratories and AbbVie for the treatment of major depressive disorder, anxiety disorders, and alcoholism but was discontinued. [1] [2] [3] It reached phase II clinical trials prior to the discontinuation of its development ...