Balovaptan (RG7314) is a novel, orally active, selective, and blood-brain barrier-penetrating vasopressin 1a (V1a) receptor antagonist[1-2]. Balovaptan regulates social behavior by antagonizing the V1a receptor, potentially improving social communication function in individuals with autism spectrum disorder. Balovaptan is applicable for research related to autism spectrum disorder[3-4].
In vivo, mice were pre-treated with an intrathecal injection of Balovaptan (0.1nmol; 5µL). Thirty minutes later, oxytocin (OT; 0.03-3nmol; 50µL) was administered subcutaneously to induce hindpaw scratching behavior. Balovaptan had a significant effect on the OT-induced scratching behavior[5]. Mice that received a single oral dose of Balovaptan (30mg/kg) were subjected to a 6-hour phase advance of their light-dark cycle. Balovaptan significantly shortened the number of days required for the circadian rhythm to resynchronize to the new cycle, thereby accelerating the re-entrainment of the circadian rhythm under simulated jet lag conditions[6].
References:
[1] Zhong P, Chu B, Yu Z, et al. Molecular basis of antagonism of the dimeric human arginine vasopressin receptor 1A. Nature Communications. 2026 Jan;17(1):1622.
[2] Ratni H, Rogers-Evans M, Bissantz C, 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.
[3] Dell'Osso L, Bonelli C, Giovannoni F, et al. Available Treatments for Autism Spectrum Disorder: From Old Strategies to New Options. Pharmaceuticals (Basel, Switzerland). 2025 Feb;18(3):324.
[4] Persico AM, Asta L, Chehbani F, et al. The pediatric psychopharmacology of autism spectrum disorder: A systematic review - Part II: The future. Progress in Neuro-psychopharmacology & Biological Psychiatry. 2025 Jan;136:111176.
[5] Guo J, Ba X, Matsuda M, et al. Oxytocin Elicits Itch Scratching Behavior via Spinal GRP/GRPR System. Front Neurosci. 2020 Sep 23;14:581977.
[6] Boareto M, Mendoza J, Holst SC, et al. Modelling the effect of V1a receptor antagonism and its potential therapeutic effect in circadian disorders. bioRxiv; 2025.
Balovaptan (RG7314)是一种新型的、具有口服活性的、选择性的、可透过血脑屏障的血管加压素1a受体拮抗剂[1-2]。Balovaptan通过拮抗V1a受体来调节社交行为，可能改善自闭症患者的社交沟通功能。Balovaptan可用于自闭症谱系障碍的相关研究[3-4]。
在体内，预先鞘内注射Balovaptan（0.1nmol；5μL）小鼠30分钟后，皮下注射催产素（OT；0.03-3nmol；50μL）诱导小鼠后爪搔抓行为。Balovaptan对OT诱导的搔抓行为产生显著影响[5]。单次口服Balovaptan（30mg/kg）处理的小鼠，在经历光照周期6小时相位提前后，Balovaptan显著缩短了节律重新同步到新周期所需的天数，加速了小鼠在时差条件下昼夜节律的重新同步[6]。