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.
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.
|
|
-
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.
|
|
-
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-0922-KX1416
|
Magic™ Human AVPR1A In Vitro Agonist & Antagonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0922-KX1419
|
Magic™ Human AVPR1A In Vitro Agonist Calcium Flux Assay
|
U2OS
|
Calcium Flux Assay
|
|
S01YF-0922-KX1423
|
Magic™ Human AVPR1A In Vitro Antagonist Calcium Flux Assay
|
U2OS
|
Calcium Flux Assay
|
|
S01YF-0922-KX1427
|
Magic™ Human AVPR1A In Vitro PAM Calcium Flux Assay
|
U2OS
|
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-0922-KX1417
|
Magic™ Human AVPR1A In Vitro Agonist & Antagonist IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-0922-KX1420
|
Magic™ Human AVPR1A In Vitro Agonist IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-0922-KX1424
|
Magic™ Human AVPR1A In Vitro Antagonist IP1 Assay
|
CHO-K1
|
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
|
|
β-Arrestin Assay
|
S01YF-0922-KX1418
|
Magic™ Human AVPR1A In Vitro Agonist β-Arrestin Assay
|
U2OS
|
β-Arrestin Assay
|
|
S01YF-0922-KX1422
|
Magic™ Human AVPR1A In Vitro Antagonist β-Arrestin Assay
|
U2OS
|
β-Arrestin Assay
|
|
S01YF-0922-KX1426
|
Magic™ Human AVPR1A In Vitro PAM β-Arrestin Assay
|
U2OS
|
β-Arrestin Assay
|
|
Internalization Assay
|
S01YF-0922-KX1421
|
Magic™ Human AVPR1A In Vitro Agonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0922-KX1425
|
Magic™ Human AVPR1A In Vitro Antagonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0922-KX1428
|
Magic™ Human AVPR1A In Vitro PAM Internalization Assay
|
U2OS
|
Internalization Assay
|
|
Radioligand Binding Assay
|
S01YF-0722-KX415
|
Magic™ Human AVPR1A In Vitro Agonist Radioligand Binding Assay
|
|
Radioligand Binding Assay
|
|
Assay No.
|
Assay Name
|
Host Cell
|
Assay Type
|
Datasheet
|
Calcium Flux Assay
|
S01YF-0922-KX1429
|
Magic™ Human AVPR1B In Vitro Agonist & Antagonist Calcium Flux Assay
|
Chem-1
|
Calcium Flux Assay
|
|
S01YF-0922-KX1433
|
Magic™ Human AVPR1B In Vitro Agonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0922-KX1437
|
Magic™ Human AVPR1B In Vitro Antagonist Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-0922-KX1441
|
Magic™ Human AVPR1B In Vitro PAM Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
S01YF-1122-KX1001
|
Magic™ Rat AVPR1B In Vitro Calcium Flux Assay
|
CHO-K1
|
Calcium Flux Assay
|
|
IP1 Assay
|
S01YF-0922-KX1430
|
Magic™ Human AVPR1B In Vitro Agonist & Antagonist IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-0922-KX1434
|
Magic™ Human AVPR1B In Vitro Agonist IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-0922-KX1438
|
Magic™ Human AVPR1B In Vitro Antagonist IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
S01YF-1122-KX1002
|
Magic™ Rat AVPR1B In Vitro IP1 Assay
|
CHO-K1
|
IP1 Assay
|
|
β-Arrestin Assay
|
S01YF-0922-KX1432
|
Magic™ Human AVPR1B In Vitro Agonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0922-KX1436
|
Magic™ Human AVPR1B In Vitro Antagonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0922-KX1440
|
Magic™ Human AVPR1B In Vitro PAM β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
Internalization Assay
|
S01YF-0922-KX1431
|
Magic™ Human AVPR1B In Vitro Agonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0922-KX1435
|
Magic™ Human AVPR1B In Vitro Antagonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0922-KX1439
|
Magic™ Human AVPR1B In Vitro PAM Internalization Assay
|
U2OS
|
Internalization 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-0922-KX1442
|
Magic™ Human AVPR2 In Vitro Agonist & Antagonist cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-0922-KX1445
|
Magic™ Human AVPR2 In Vitro Agonist cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-0922-KX1448
|
Magic™ Human AVPR2 In Vitro Antagonist cAMP Assay
|
CHO-K1
|
cAMP Assay
|
|
S01YF-0922-KX1451
|
Magic™ Human AVPR2 In Vitro PAM cAMP Assay
|
CHO-K1
|
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
|
|
β-Arrestin Assay
|
S01YF-0922-KX1444
|
Magic™ Human AVPR2 In Vitro Agonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0922-KX1447
|
Magic™ Human AVPR2 In Vitro Antagonist β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
S01YF-0922-KX1450
|
Magic™ Human AVPR2 In Vitro PAM β-Arrestin Assay
|
CHO-K1
|
β-Arrestin Assay
|
|
Internalization Assay
|
S01YF-0922-KX1443
|
Magic™ Human AVPR2 In Vitro Agonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0922-KX1446
|
Magic™ Human AVPR2 In Vitro Antagonist Internalization Assay
|
U2OS
|
Internalization Assay
|
|
S01YF-0922-KX1449
|
Magic™ Human AVPR2 In Vitro PAM Internalization Assay
|
U2OS
|
Internalization Assay
|
|
Radioligand Binding Assay
|
S01YF-0722-KX417
|
Magic™ Human AVPR2 In Vitro Agonist Radioligand Binding Assay
|
|
Radioligand Binding 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.
Fig.2. Localization of V-receptors and sodium transport systems in the kidney. (Natochin & Golosova, 2020)
|
References
-
Demiselle, J.; et al. Vasopressin and its analogues in shock states: a review. Annals of intensive care. 2020, 10(1): 1-7.
-
Natochin, Y.V.; Golosova, D.V. Vasopressin receptor subtypes and renal sodium transport. Vitamins and Hormones. 2020, 113: 239-258.
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