Introduction of AVPR1B

The effects of vasopressin are mediated through stimulation of vasopressin receptors. So far, three vasopressin receptor subtypes have been identified, one of them is the AVPR1B receptor (also known as V1b). V1b belongs to the subfamily of G-protein coupled receptors. Upon stimulation of the V1a receptor by AVP, a Gq-phospholipase C-inositol trisphosphate pathway is activated, leading to elevation of the intracellular Ca²⁺ concentration and activation of protein kinase C. These intracellular signaling molecules elicit biological outcomes including vasoconstriction, glycogenolysis, platelet activation, and release of adrenocorticotropic hormone. This receptor is distributed in the anterior pituitary, pancreas, adrenal medulla, white adipose tissue, and the CNS.

Functions of AVPR1B Membrane Protein

Genetic deletion of the V1b receptor lowers stress responses in mice. Pharmacological tools have been developed to investigate the role of this receptor in stress and anxiety. The treatment of V1b receptor antagonists has exhibited anxiolytic-like effects in rodents. Besides, V1b receptor knockout mice have also revealed that this receptor may be, at least in part, involved in body water balance and body temperature regulation. Moreover, AVPR1B null mutant mice are impaired in the modulation of ultrasonic vocalizations within different social contexts at infant and adult ages. In addition, V1b receptor polymorphism is associated with bipolar disorder. However, more specific functions of V1b receptor remains to be established.

Fig.1 Human V1b receptor. (Koshimizu, 2012)

Applications of AVPR1B Membrane Protein in Literature

1. Ishizuka Y., et al. Involvement of vasopressin V1b receptor in anti-anxiety action of SSRI and SNRI in mice. Neuroscience Research. 2010, 66(3): 233-237. PMID: 19914307

This study investigated the effects of treatment with a selective serotonin reuptake inhibitor (SSRI) and with a serotonin-noradrenalin reuptake inhibitor (SNRI) on V1b receptor-deficient mice and on v1b receptor antagonist (SSR149415)-treated mice. The results suggested the involvement of V1b receptor in regulating the anxiety behaviors.

2. Hodgson R A., et al. Characterization of a novel vasopressin V1b receptor antagonist, V1B-30N, in animal models of anxiety-like and depression-like behavior. European Journal of Pharmacology. 2014, 730(1): 157-163. PMID: 24602808

This study assessed the antidepressive-like properties of V1B-30N in mouse and rat models of anxiety. The results showed that the acute pharmacological antagonism of the V1b receptor had anxiolytic-like but not antidepressant-like properties.

3. Corbani M., et al. Neuroanatomical distribution and function of the vasopressin V1B receptor in the rat brain deciphered using specific fluorescent ligands. Gen Comp Endocrinol. 2017, 258: 15-32. PMID: 29155265

This study determined the pharmacological properties of three new potent rat V1b fluorescent ligands and demonstrated that they constituted valuable tools for simultaneous visualization and activation of native V1b receptors in living rat brain tissue.

4. Qi X., et al. Chronic treatment with the vasopressin 1b receptor antagonist SSR149415 prevents the dysphoria associated with nicotine withdrawal in rats. Behavioural Brain Research. 2015, 292: 259-265. PMID: 26112757

This study investigated the effect of acute and chronic treatment with the V1b receptor antagonist SSR149415 on the negative mood state associated with nicotine withdrawal in rats. The results suggested that chronic treatment with V1b receptor antagonists may prevent the dysphoria associated with smoking cessation and thereby improve relapse rates.

5. Bayerl D S., et al. Antagonism of V1b receptors promotes maternal motivation to retrieve pups in the MPOA and impairs pup-directed behavior during maternal defense in the mpBNST of lactating rats. Hormones and behavior. 2016, 79: 18-27. PMID: 26747375

This study demonstrated that V1bR antagonism significantly modulated different aspects of maternal behavior in a brain region-dependent manner.

AVPR1B Preparation Options

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Reference

1. Koshimizu, T. A., et al. (2012). Vasopressin v1a and v1b receptors: from molecules to physiological systems. Physiological Reviews. 92(4), 1813-64.

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