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Vasopressin GPCR Assays

Background of Vasopressin Receptors

Vasopressin receptors belong to the family of G protein-coupled receptors (GPCR). The Vasopressin receptors mediate various biological functions, such as vasoconstriction, antidiuresis, and adrenocorticotropic hormone (ACTH) release.

Physiological effects of vasopressin. Fig.1. Physiological effects of vasopressin. (Demiselle, 2020)

Distributions and Functions of Vasopressin Receptors

AVPR1A is found in high density on vascular smooth muscle and induces various biological functions, such as vasoconstriction, facilitating thrombosis, and stimulating VEGF secretion. AVPR1B located in the hypothalamus controls ACTH secretion, while AVPR1B located in the pancreas is involved in insulin release. The expression of AVPR2V2 can only be found on the basolateral membrane of collecting duct cells in the kidney, for the regulation of water excretion.

Subtypes and Mechanisms of Vasopressin Receptors

There are three subtypes of vasopressin receptors, including arginine vasopressin receptor 1A (AVPR1A), Arginine vasopressin receptor 1B (AVPR1B), and Arginine vasopressin receptor 2 (AVPR2).

Receptor Gene Mechanism Agonists Antagonists
Arginine vasopressin receptor 1A AVPR1A
  • Arginine vasopressin receptor 1A couples to Gq/11 proteins for the regulation of blood pressure through arterial vasoconstriction.
  • Arginine vasopressin stimulation induces an increase in intracellular calcium, facilitating thrombosis.
  • [Phe2, Ile3, Orn8]-vasopressin
  • Phe2OVT
  • Conivaptan hydrochloride
  • OPC 21268
  • SR 49059
  • TC OT 39
Arginine vasopressin receptor 1B AVPR1B
  • Arginine vasopressin receptor 1B activates several signaling pathways via different G-proteins.
  • Desmopressin
  • OPC 21268
  • SSR 149415
  • TASP 0390325
Arginine vasopressin receptor 2 AVPR2
  • Arginine vasopressin receptor 2 couples with Gs proteins for the regulation of water excretion.
  • Desmopressin
  • TC OT 39
  • Conivaptan hydrochloride
  • Tolvaptan

Assay List of Vasopressin Receptors

Creative Biolabs can provide a range of assays of vasopressin receptors. You can choose the assay in the list or contact us for more information:

AVPR1A AVPR1B AVPR2
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX994 Magic™ Mouse AVPR1A In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX995 Magic™ Rabbit AVPR1A In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX996 Magic™ Rat AVPR1A In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-1122-KX989 Magic™ Dog AVPR1A In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
S01YF-0722-KX202 Magic™ Cynomolgus AVPR1A In Vitro Calcium Assay & Binding Assay, CHO-K1 CHO-K1 Calcium Assay; Binding Assay
IP1 Assay
S01YF-1122-KX997 Magic™ Rat AVPR1A In Vitro IP1 Assay CHO-K1 IP1 Assay
S01YF-1122-KX990 Magic™ Dog AVPR1A In Vitro IP1 Assay CHO-K1 IP1 Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX1001 Magic™ Rat AVPR1B In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
IP1 Assay
S01YF-1122-KX1002 Magic™ Rat AVPR1B In Vitro IP1 Assay CHO-K1 IP1 Assay
Radioligand Binding Assay
S01YF-1122-KX1000 Magic™ Human AVPR1B In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
S01YF-1122-KX1003 Magic™ Rat AVPR1B In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay
Assay No. Assay Name Host Cell Assay Type Datasheet
cAMP Assay
S01YF-1122-KX1009 Magic™ Rat AVPR2 In Vitro cAMP Assay CHO-K1 cAMP Assay
S01YF-1122-KX1004 Magic™ Dog AVPR2 In Vitro cAMP Assay CHO-K1 cAMP Assay
Calcium Flux Assay
S01YF-1122-KX1005 Magic™ Human AVPR2 In Vitro Calcium Flux Assay CHO-K1 Calcium Flux Assay
IP1 Assay
S01YF-1122-KX1007 Magic™ Human AVPR2 In Vitro IP1 Assay CHO-K1 IP1 Assay

Published Data

Paper Title Vasopressin receptor subtypes and renal sodium transport
Journal Vitamins and Hormones
Published 2020
Abstract In mammals, three V receptor subtypes have been identified in the kidney. Three different receptor subtypes, V2, V1a, and V1b, trigger vasopressin, a hormone synthesized in the hypothalamus. Stimulation of V2 receptors can modulate urine osmolarity. Stimulation of V1a receptors inhibits renal sodium reabsorption and induces urinary sodium excretion. Stimulation of V1b receptors induces potassium secretion in the final part of the distal segment and the initial part of the collecting duct. In this paper, we describe the interaction of vasopressin with V receptor subtypes to better understand the role of these systems and their regulation in facilitating the identification of other systemic components and mechanisms.
Result Physiologically, it is important to simultaneously characterize the characteristics and capabilities of each Na+ transport system in the renal tubule and their roles under conditions of different functional states of the organism. We already know that the involvement of various subtypes of V receptors plays a key role in stabilizing the physicochemical parameters of the human internal environment and water-salt homeostasis. Increased renal Na+ excretion is involved in osmotic homeostasis mechanisms when serum Na+ concentrations are elevated and arginine vasopressin (AVP) levels are elevated. This suggests that V1aR and V2R are activated under hypernatremia. Furthermore, the mode by which AVP regulates water and Na+ transport is physiologically appropriate under conditions of dehydration. Vasopressin is a unique physiologically active substance that stimulates different subtypes of V receptors and maintains extracellular fluid volume and osmolarity. It may be developed as a novel therapeutic agent to promote water-salt homeostasis.

Localization of V-receptors and sodium transport systems in the kidney.Fig.2. Localization of V-receptors and sodium transport systems in the kidney. (Natochin & Golosova, 2020)

References

  1. Demiselle, J.; et al. Vasopressin and its analogues in shock states: a review. Annals of intensive care. 2020, 10(1): 1-7.
  2. Natochin, Y.V.; Golosova, D.V. Vasopressin receptor subtypes and renal sodium transport. Vitamins and Hormones. 2020, 113: 239-258.
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