AVPR1A Membrane Protein Introduction

Introduction of AVPR1A

AVPR1A belongs to a family of heptahelical guanine nucleotide-binding protein-coupled receptors (GPCRs). It is also known as the V1a vasopressin receptor which functions by binding to the neurohypophysial hormone arginine vasopressin (AVP). It is a 418-amino acid protein linked to the phosphoinositol signaling pathway. AVP binding to the receptor causes activation of Gq/11-mediated phospholipase C, resulting in an increase in intracellular calcium. The V1a receptor is expressed in a variety of tissues including vascular smooth muscle, cardiac myocytes, brain, testis, the superior cervical ganglion, liver, platelets, and the renal medulla.

Functions of AVPR1A Membrane Protein

V1a receptor knockout mice were used to evaluate the functional role of this receptor in regulating vascular tonus and blood pressure. The results showed that the V1a receptor was responsible for AVP-induced vascular contraction and that the V1a receptors seem to be necessary for maintaining the basal BP. Furthermore, in the central nervous system, AVP plays a crucial role in regulating cardiovascular homeostasis via the V1a receptor. In water reabsorption, the V1a receptor is responsible for natriuresis at high doses of AVP. Besides, V1a receptors in the kidney have been proposed to play a role in 1) inhibitory regulation of the basolateral V2 receptor-mediated antidiuretic and antinatriuretic action of AVP and 2) regulation of renin production in the MD cells, and 3) regulation of aldosterone action on H⁺-ATPase, H⁺-K⁺-ATPase, and Rhcg in the intercalated cells. additionally, AVP also modulates the balance of other metabolic functions, such as cellular growth and proliferation, protein turnover, lipid metabolism, and glucose handling via V1a or V1b receptors.

Fig.1 Human V1a receptor. (Koshimizu, 2012)

Applications of AVPR1A Membrane Protein in Literature

1. Żera T., et al. Vasopressin V1a receptors are present in the carotid body and contribute to the control of breathing in male Sprague-Dawley rats. Peptides. 2018, 102: 68-74. PMID: 29524562

This study investigated if carotid bodies contain V1aRs and how the receptors were involved in the regulation of ventilation by AVP. The results showed chemosensory cells within carotid bodies expressed V1a receptors and that it was involved in the control of breathing.

2. Everett N A., et al. The role of the vasopressin V1A receptor in oxytocin modulation of methamphetamine primed reinstatement. Neuropharmacology. 2018, 133: 1-11. PMID: 29353054

This article investigated the involvement of the V1AR in mediating the effect of oxytocin treatment to reduce methamphetamine (METH)-primed reinstatement of METH-seeking behavior. The results showed that V1a receptor played an important role in mediating the inhibitory effects of oxytocin on METH-primed reinstatement.

3. Duque-Wilckens N., et al. Inhibition of vasopressin V1a receptors in the medioventral bed nucleus of the stria terminalis has sex- and context-specific anxiogenic effects. Neuropharmacology. 2016, 110(Pt A): 59-68. PMID: 27452721

This studied the effects of sex and social defeat stress on V1aR binding in the forebrain using the California mouse. The data suggested that V1aR in medioventral BNST (BNSTmv) had anxiolytic and prosocial effects in males and that in females, prosocial and anxiolytic effects of V1aR appeared to be mediated independently by receptors in the BNSTmv and NAc shell, respectively.

4. Bayerl D S., et al. Vasopressin V1a, but not V1b, receptors within the PVN of lactating rats mediate maternal care and anxiety-related behavior. Behavioural Brain Research. 2016, 305: 18-22. PMID: 26909846

This study investigated the role of both V1aR and V1bR within the hypothalamic paraventricular nucleus (PVN) of lactating rats. The results demonstrated that AVP acted mainly via V1aR in the PVN to mediate maternal care and anxiety.

5. Lozić M., et al. Over-expression of V1A receptors in PVN modulates autonomic cardiovascular control. Pharmacological Research. 2016, 114: 185-195. PMID: 27810519

This study investigated the role of the V1a receptor in the hypothalamic paraventricular nucleus (PVN) in cardiovascular control in response to stress. The results suggested a possible role of the hypothalamic V1a receptor in cardiovascular pathology.

AVPR1A 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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