trpv3

TRPV3 antagonist 74a (TRPV3 74a) 是一种特异性 TRPV3 拮抗剂，可用于研究神经系统相关疾病。

N-Oleoyl Valine Ammonium salt 是一种 N- 酰基酰胺化合物，是一种 TRPV3 拮抗剂，可用于研究炎症。

(+)-Camphor (D-Camphor) 是一种食品添加剂，在医学上可用作防腐剂。

2-Aminoethyl diphenylborinate (2-APB) 是细胞通透性的 IP3R 和 TRP 通道抑制剂，还抑制 store-operated Ca2+(SOC)通道。

beta-Eudesmol (Beta-Selinenol) 是天然的含氧倍半萜烯，可激活hTRPA1，EC50值为 32.5 μM。Beta-Eudesmol 有增加食欲的功效。

Resolvins are a family of potent lipid mediators derived from both eicosapentaenoic acid and docosahexaenoic acid.[1] In addition to being anti-inflammatory, resolvins promote the resolution of the inflammatory response back to a non-inflamed state.[2] Resolvin D1 is produced physiologically from the sequential oxygenation of DHA by 15- and 5-lipoxygenase.[1] 17(R)-RvD1 is an aspirin-triggered epimer of RvD1 that reduces human polymorphonuclear leukocyte (PMN) transendothelial migration, the earliest event in acute inflammation, with equipotency to RvD1 (EC50 = ~30 nM).[3] 17(R)-RvD1 exhibits a dose-dependent reduction in leukocyte infiltration in a mouse model of peritonitis with maximal inhibition of ~35% at a 100 ng dose.[3] In contrast to RvD1, the aspirin-triggered form resists rapid inactivation by eicosanoid oxidoreductases. Analytical and biological comparisons of synthetic 17(R)-RvD1 with endogenously derived 17(R)-RvD1 have confirmed its identity as matching the natural product.[4]

N-Oleoyl valine is an endogenous N-acyl amine that acts as an antagonist at the transient receptor potential vanilloid type 3 (TRPV3) receptor, which is involved in thermoregulation. N-Oleoyl valine is increased in mice following cold exposure for up to at least 16 days. Acute lung injury in mice increases the concentration of N-Oleoyl valine in lung tissue. N-acyl amines also promote mitochondrial uncoupling.

Bisandrographolide C is identified from Andrographis paniculata. Bisandrographolide C activates TRPV1 and TRPV3 channels (Kds: 289 and 341 μM) and protects cardiomyocytes from hypoxia-reoxygenation injury.

Carvone is an agonist of TRPV3 found in spearmint oil. It suppresses cell proliferation in prostate cancer cells and inhibits the growth of Dermatophagoides.

SET 2 是瞬时受体电位香草酸 2 型 (TRPV2) 的拮抗剂，IC50 为 0.46 μM。 SET 2 显示了对 TRPV1、TRPV3 和 TRPV4 的选择性。

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).

TRPV2-selective blocker 1 (compound IV2-1) 为选择性TRPV2通道阻断剂，具有6.3 μM IC50，不对TRPV1、TRPV3和TRPV4通道产生影响。该化合物能够抑制巨噬细胞中TRPV2介导的Ca2+流入，进而抑制其吞噬功能。