et al. Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB223412, a novel, potent and selective neurokinin-3 receptor antagonist. J. Pharmacol. Exp. Ther. 281, 1303?1311 (1997). CAS PubMed Google Scholar Almeida, T. A. et al. Tachykinins...
Although the discovery of potent and selective nonpeptide NK 3 receptor antagonists initially lagged behind the development of comparable molecules for NK l and NK 2 receptors, work in this field has rapidly progressed. Both selective and nonselective antagonist s displaying nanomolar potencies for ...
4.Simon, JA; Anderson, RA; Ballantyne, E, et al. (2023). Efficacy and safety of elinzanetant, a selective neurokinin-1,3 receptor antagonist for vasomotor symptoms: a dose-finding clinical trial (SWITCH-1). Menopau...
Update NK3R-Antagonist Fezolinetant Originalpublikation Santoro N et al (2020) Effect of the neurokinin 3 receptor antagonist fezolinetant on patient-reported outcomes in postmenopausal women with vasomotor symptoms: results of a randomized, placebo-controlled, double-blind, dose-ranging study (VESTA...
Osanetant | NK3 拮抗剂,Osanetant - SR 142801CAS160492-56-8C35H41Cl2N3O2 MW 606.64 Purity: >98% (optically pure)Biological Activity: Potent non-peptide neurokinin3 (NK3) receptor antagonist.References: X Emonds-Alt et al.
Fezolinetant, also known as ESN-364, is Neurokinin-3 (NK-3) receptor antagonist which has been optimized for use in women’s health, and is being developed for sex-hormone related disorders such as endometriosis, polycystic ovarian syndrome and uterine f
代理机构: 代理人: 地址: 摘要: This invention relates to the treatment or prevention of nausea and/or vomiting by the administration of a NK-3 receptor antagonist. 二、法律状态 暂无信息 三、权利要求 暂无信息 四、说明书暂无信息 打开APP,查看更多专利的权利要求、说明书更多...
elicitedalower maximalresponse(7.5±0.8and8.1±0.6%ofthetotallobularamylasecontent)thancarbachol(34.4±3.9%),caerulein(26.5±2.8%) andKCl(22.5±3.8%).WhereasatropineleftPG-KIIandsenktide-stimulatedsecretionunaffected,thenonpeptideNK 3 receptorantagonist SR142801significantlyreducedthestimulanteffectofPG-...
The new compounds are also far more stable from a metabolic point of view than the known peptidic NK-3 receptor antagonists and are of potential therapeutic utility. The new compounds also have good NK-2 antagonist activity and are therefore considered to be of potential use in the prevention ...
Treatment of Menopausal Vasomotor Symptoms With Fezolinetant, a Neurokinin 3 Receptor Antagonist: A Phase 2a Trial Context: The thermoregulatory center in the hypothalamus is stimulated by neurokinin 3 receptor (NK3R) activation and inhibited by estrogen-negative feedback. This balance is disrupted in...