Balovaptan (RG7314) (RG7314) 是一种口服有效的选择性脑渗透性血管加压素 1a (hV1a) 受体拮抗剂，对人类 (hV1a) 和小鼠 (mV1a) 受体的 Kis 分别为 1 和 39 nM，用于研究自闭症。
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for hV1a and mhV1a, and is used for the research of autism. Balovaptan shows >30000-fold selectivity for hV1a over hV2 receptors, 9891-fold selectivity over hOTR (human oxytocin receptor)[1].
[1]. Ratni H, et al. Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem. 2015 Mar 12;58(5):2275-89.
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