1. Signaling Pathways
  2. GPCR/G Protein
  3. Vasopressin Receptor

Vasopressin Receptor (血管加压素受体)

神经垂体激素精氨酸加压素 (AVP) 参与多种功能,包括调节体液稳态、血管收缩和促肾上腺皮质激素释放。这些生理效应由三种亚型的加压素受体介导,即 V1a、V1b(或 V3)和 V2。它们都属于大型视紫红质样 G 蛋白偶联受体家族。

V1a 受体在包括心脏在内的神经元和非神经元组织中均有表达,并引发多种生理效应,包括细胞收缩和增殖、刺激肝糖原分解、血小板聚集和凝血因子释放。V1b 受体亚型主要存在于脑垂体中,可刺激促肾上腺皮质激素的释放。V1a 和 V1b AVP 受体均通过 Gαq 家族 (αq、q11、q14、α15/16) 的 G 蛋白 α 亚基起作用,以激活磷脂酶 C-β,从而提高细胞 IP3 和钙水平。相比之下,V2 受体亚型主要位于肾脏,通过异三聚体 G 蛋白 Gs 和腺苷酸环化酶的激活介导 AVP 的抗利尿作用。

The neurohypophysial hormone arginine vasopressin (AVP) is involved in diverse functions including regulation of body fluid homeostasis, vasoconstriction, and adrenocorticotropic hormone release. These physiological effects are mediated by three subtypes of vasopressin receptors, designated V1a, V1b (or V3), and V2. They all belong to the large rhodopsin-like G-protein-coupled receptor family.

The V1a receptor is expressed in both neuronal and non-neuronal tissues including the heart and elicits a variety of physiological effects including cell contraction and proliferation, stimulation of hepatic glycogenolysis, platelet aggregation and coagulation factor release. The V1b receptor subtype is found predominantly in the pituitary gland where it stimulates adrenocorticotropic hormone release. Both the V1a and V1b AVP receptors act through a G protein alpha-subunit of the Gαq family (αq, q11, q14, α15/16) to activate phospholipase C-β, and, thus enhance cellular IP3 and calcium levels. By contrast, the V2 receptor subtype is localized predominantly to the kidney where it mediates the anti-diuretic effects of AVP through the heterotrimeric G protein Gs and activation of adenylyl cyclase.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P0041
    F992 Inhibitor
    F992 是一种抗利尿肽和后叶加压素 (抗利尿激素) 类似物。
    F992
  • HY-172814A
    OT-R agonist 1 TFA Antagonist
    OT-R agonist 1 TFA (compound 5) 是一种催产素受体 (oxytocin receptor ) 激动剂,其 EC50 值为 0.39 nM。 OT-R agonist 1 TFA 显示 V1A 拮抗剂活性,EC50 值为 2432 nM,可用于研究中枢神经系统疾病的研究。
    OT-R agonist 1 TFA
  • HY-19880
    RWJ-676070 Antagonist
    RWJ-676070 是一种双重加压素 V(1A)/V(2) 受体拮抗剂,其 Ki 值分别为 1.4 nM 和 14 nM。
    RWJ-676070
  • HY-P1747
    Pneumadin, rat
    Pneumadin, rat (PNM) 是一种十肽, 对精氨酸加压素 (AVP) 的释放具有有效的刺激作用。Pneumadin, rat (PNM) 对有功能性 AVP 系统的动物有明显的抗利尿作用。
    Pneumadin, rat

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