human trpv1

A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.

Oleoyl Serotonin 是 hTRPV1 的拮抗剂，IC50（Human TRPV1） 为 2.57 μM。

OMDM-5 是有效的、选择性的anandamide 细胞摄取抑制剂，Ki 为 4.8 μM。它是VR1 (TRPV1)激动剂，EC50为 75 nM，显示出对大麻素 1 型受体 (CB1) 的弱配体活性 (Ki=4.9 μM)。

A-889425 是一种口服选择性TRPV1受体拮抗剂，其 IC50 值为335 nM（大鼠）和34 nM（人）。该化合物能有效渗透中枢神经系统，能减轻机械性异常痛，并降低脊髓神经元对 Complete Freund's adjuvant 引起的炎症大鼠后爪机械刺激的敏感性。

DWP-05195 作为一种TRPV1拮抗剂，具有抑制疼痛信号转导的能力。此外，DWP-05195 还能通过 ROS-p38-CHOP 通路在人类卵巢癌细胞中引发 ER 应激依赖性细胞凋亡。

MDR-652是瞬时受体电位香草酸亚型 1 的选择性激动剂，对 hTRPV1 和 rTRPV1 的Ki 分别为 11.4 和 23.8 nM，EC50分别为 5.05 和 93 nM。MDR-652在缓解疼痛方面有研究的价值。

RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays). |1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg. Med. Chem. Lett. 25(18), 4011-4015 (2015).

TRPV1 antagonist 3 (Compound 7q) is a highly potent antagonist of the TRPV1 receptor with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity towards its mode of action and is orally bioavailable (with a bioavailability of 60%). Additionally, it can penetrate the central nervous system [1].

SB705498 是一种口服有效的 TRPV1选择性拮抗剂，pIC50值为 7.1。

AMG9810是高效的，竞争性的香草素受体1选择性拮抗剂，对人类和大鼠TRPV1的IC50分别为24.5 和 85.6 nM。

PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。

JNJ-17203212 是一种竞争性 TRPV1选择性拮抗剂。它被开发用于疼痛处理的研究。

Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.

Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late