gepant

Vazegepant hydrochloride (Vazegepant HCl) 是一种用于偏头痛的鼻用 gepant，是一种高度亲和性CGRP 受体拮抗剂 (hCGRPKi=0.023 nM)。它可能有助于有效管理 COVID-19 相关肺部炎症。

Rimegepant (BMS 927711) 是一种有效的降钙素基因相关肽 (CGRP) 受体拮抗剂 (Ki=0.027 nM，IC50=0.14 nM)。Rimegepant 可同时用于偏头痛急性发作治疗及预防性治疗。

Atogepant (MK-8031) 是一种可口服且具有选择性和高效性的降钙素基因相关肽受体 (CGRP) 拮抗剂，可用于研究偏头痛。

Olcegepant hydrochloride (奥塞吉泮盐酸盐，BIBN-4096 hydrochloride)是一种选择性的降钙素基因相关肽1 (CGRP1) 受体拮抗剂，IC50=0.03 nM，Ki=14.4 pM。

Olcegepant (BIBN-4096) 是一种选择性的降钙素基因相关肽1 (CGRP1) 受体拮抗剂，IC50=0.03 nM，Ki=14.4 pM。

Telcagepant（MK-0974，替卡吉泮）是一种口服的降钙素基因相关肽受体（CGRP, calcitonin gene-related peptide）拮抗剂，阻断CGRP受体并减少中枢神经系统的神经传递，用于研究偏头痛和减轻疼痛。

Ubrogepant (MK-1602) 是新型的、口服有效的降钙素基因相关肽受体拮抗剂。Ubrogepant 有潜力用于急性偏头痛的相关研究。

Vazegepant (Zavegepant) 是一种可口服且具有选择的降钙素基因相关肽 CGRP 受体拮抗剂，可缓解疼痛，可用于研究偏头疼。

Rimegepant, also known as BMS-927711 and BHV-3000, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraines. Rimegepant has shown in vivo efficacy without vasoconstriction effect. BMS-927711 is superior to placebo at several different doses (75 mg, 150 mg, and 300 mg) and has an excellent tolerability profile.

(3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) 是Atogepant 的异构体.Atogepant 是降钙素基因相关肽受体 (CGRP) 拮抗剂。Atogepant 可用于研究偏头痛。

C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mechanical allodynia and inflammation. C3001a represents a lead compound which could advance the rational design of peripherally acting analgesics targeting K2P channels without opioid-like adverse effects.