Fezolinetant是一种神经激肽-3受体(neurokinin3receptor)拮抗剂，可用于更年期潮热的研究。
CAS：1629229-37-3
分子式：C16H15FN6OS
分子量：358.39
纯度：98%
存储：Store at -20°C

Background:

Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

Fezolinetant (ESN364, 1 mg/kg, iv bolus) reversibly inhibits the regular, pulsatile secretion of LH in the ovarectomized ewe. ESN364 represses the pulse pattern of LH in all treated animals. ESN364 (5 mg/kg, p.o.) lowers plasma LH, but not FSH, in the castrated monkey. ESN364 (10, 25, 50 mg/kg, orally) also blocks the LH surge and decreases ovarian hormone levels throughout the menstrual cycle in monkeys[1].

[1]. Fraser GL, et al. The NK3 Receptor Antagonist ESN364 Interrupts Pulsatile LH Secretion and Moderates Levels of Ovarian Hormones Throughout the Menstrual Cycle. Endocrinology. 2015 Nov;156(11):4214-25.