vr1

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)。

Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。

OMDM-1 ((Z)-N-[(2S)-1-hydroxy-3-(4-hydroxyphenyl)propan-2-yl]octadec-9-enamide) 是有效选择性的代谢稳定 anandamide 细胞摄取抑制剂，Ki=为2.4 μM。

SB366791 是一种有效的 vanilloid receptor (VR1 TRPV1)选择性拮抗剂 (IC50=5.7 nM)。SB-366791 在炎症方面有研究价值。

DD-161515 is a VR1 antagonist.

vanilloid TRPV1 (VR1) receptor agonist

CEDAEVFKDSMVPGEK 为大鼠辣椒素受体亚型 1 (VR1) 的多肽序列片段，适用于探测 VR1 的存在、分布及分子形态。

Several different arachidonoyl amino acids, including N-arachidonoyl-L-alanine (NALA), have been isolated and characterized from bovine brain. The glycine congener (NAGly) was further characterized and found to suppress formalin-induced pain in rats. NALA may have activity at cannabinoid receptor and/or VR1, but has not been fully characterized to date.

TRPV1 (VR1) receptor antagonist

TRPV1 (VR1) vanilloid receptor partial agonist

Cannabinoid CB1 and vanilloid TRPV1 (VR1) agonist

N-Arachidonoyl-L-serine (ARA-S), a recently isolated endocannabinoid with a distinct activity profile that diverges from typical endocannabinoids, does not interact with central cannabinoid (CB1), peripheral cannabinoid (CB2) receptors, or vanilloid receptor 1 (VR1). Unlike other compounds, ARA-S (5 mg kg) counteracts the lowering of blood pressure induced by a 10 mg kg intravenous bolus of abnormal cannabidiol (Abn-CBD) in anesthetized rat models. Additionally, akin to Abn-CBD, ARA-S induces relaxation in isolated rat mesenteric arteries and abdominal aorta and promotes phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in human umbilical vein endothelial cells (HUVEC). The mechanisms through which ARA-S and Abn-CBD exert their effects on vascular systems show variations and merit deeper investigation.

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.

Vanilloid TRPV1 (VR1) receptor antagonist peptide (IC50 ~ 0.1 μM); blocks Ca2+ currents in dorsal root ganglion neurons. Analgesic in vivo.

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。