NBI-98782 is a potent and selective vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki value of 3nM [1]. NBI-98782 reduces the packaging of monoamines by targeting VMAT2, thereby leading to a decrease in monoamine release and neural transmission[2]. NBI-98782 has been widely used to promote ptosis in rats, stimulate prolactin secretion, and regulate neural functions[3].
In vivo, NBI-98782 treatment via oral administration at a dose of 10mg/kg/day for 7 days significantly decreased basal levels of dopamine and serotonin, and enhanced the release of acetylcholine and GABA levels in mice [4].
References:
[1] Meyer J M. Valbenazine for tardive dyskinesia[J]. Curr Psychiatr, 2017, 16(5): 40-46.
[2] Terry-Lorenzo R, Albrecht D, Crouch S, et al. Quantifying VMAT2 target occupancy at effective valbenazine doses and comparing to a novel VMAT2 inhibitor: a translational PET study[J]. Neuropsychopharmacology, 2025, 50(7): 1093-1101.
[3] Grigoriadis D E, Smith E, Hoare S R J, et al. Pharmacologic characterization of valbenazine (NBI-98854) and its metabolites[J]. The Journal of Pharmacology and Experimental Therapeutics, 2017, 361(3): 454-461.
[4] Huang M, He W, Rajagopal L, et al. Effects of NBI-98782, a selective vesicular monoamine transporter 2 (VMAT2) inhibitor, on neurotransmitter efflux and phencyclidine-induced locomotor activity: Relevance to tardive dyskinesia and antipsychotic action[J]. Pharmacology Biochemistry and Behavior, 2020, 190: 172872.
NBI-98782是一种强效且选择性的vesicular monoamine transporter 2 (VMAT2)抑制剂，Ki值为3nM[1]。NBI-98782通过靶向VMAT2减少单胺的包装，从而导致单胺释放和神经传递减少[2]。NBI-98782已被广泛用于诱导大鼠上睑下垂、刺激催乳素分泌和调节神经功能[3]。
在体内，通过口服给予10mg/kg/day剂量的NBI-98782处理7天，显著降低了小鼠的多巴胺和血清素基础水平，并增强了乙酰胆碱的释放和GABA水平[4]。