hv1a

Balovaptan (RG7314) 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. It is used for the research of autism.

ω-Hexatoxin-Hv1a, a neurotoxin extracted from the venom of the spider Hadronyche versuta, inhibits voltage-gated calcium channels [1] [2].

RG7713 (RO 5028442) has been used in trials studying Autistic Disorder.

V1a V2 antagonist 1 (Compound 18j) is an orally active dual-target antagonist of V1a and V2 receptors, exhibiting high binding affinity toward these receptors [Ki values are hV1a: 0.13 nM, hV2: 0.53 nM, and mV1a: 0.5 nM; IC50 for hV1a is 2.2 nM]. This compound can inhibit oxytocin-induced scratching behavior in mice.

RGH-122 (compound 43), characterized as an orally active, potent, and selective hV1a receptor antagonist, demonstrates significant affinity with a K i value of 0.3 nM and an IC 50 of 0.9 nM. It exhibits microsomal stability, indicated by a CL int value of 13/28/25 μL/min/mg [1].