vanilloid receptor antagonist-1

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) 是香草酸受体的有效拮抗剂。

ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂，也是一种TRPV1拮抗剂。

ABT 102 (CHEMBL398338) 是瞬时受体电位香草素 1 (TRPV1) 受体的选择性拮抗剂。

TRPV antagonist 1 is an antagonist of transient receptor potential vanilloid (TRPV; IC50 < 250 nM).

GSK3395879 is a selective and orally bioavailable antagonist of transient receptor potential vanilloid-4 (TRPV4) (IC50: 1 nM for hTRPV4).

Asivatrep (PAC14028) 是一种具有选择性和高效性的瞬时受体电位香草酸亚型1 (TRPV1) 拮抗剂，可用于研究特应性皮炎。

SB 452533 是TRPV1的选择性拮抗剂，pKb 为 7.8。

AS1928370 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).

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).

Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Capsaicin signals are transduced by a heat-activated ion channel, the vanilloid receptor 1 (VR1), or transient receptor potential vanilloid 1 (TRPV1). CAY10448 is an iodinated nonivamide, a potent capsaicin receptor antagonist with an IC50 value of approximately 10 nM.

Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant. Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 |Gavva et al (2007) The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J.Neurosci. 27 3366 PMID:17392452

JTS-653 is a potent and selective in vitro and in vivo antagonist of transient receptor potential vanilloid 1 (TRPV1). It effectively attenuates chronic pain resistant to non-steroidal anti-inflammatory drugs.

JNJ-38893777 is a potent and selective transient receptor potential vanilloid 1 (TRPV1) channel antagonist.

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。

L-R4W2 TFA，作为一种有效的香草酸受体1 (VR1，TRPV1) 拮抗剂，其IC50值达到0.1 μM，主要用于疼痛缓解的研究。

TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时，它能增加大鼠后爪机械痛阈。

α-Spinasterol 是一种从Spinacia oleracea 分离的瞬时受体电位香草酸 1 拮抗剂，具有抗菌、抗炎、抗抑郁、抗氧化和抗伤害作用。它抑制COX-1和COX-2活性，IC50值分别为 16.17 μM 和 7.76 μM。