vr1

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-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)。

VR17-04，Enisamium的一种代谢产物，能够阻止在RNA合成过程中GTP与UTP的嵌入。通过对接和分子动力学模拟揭示了其作用机制。这些研究成果表明，VR17-04可作为管理COVID-19的潜在抗病毒策略。

IC50 为 0.24 μMIHVR-17028 是一种有效的广谱的 ER α-葡萄糖苷酶 I (α-glucosidase I) 抑制剂，IC50 为 0.24 μM，具有抗病毒活性。 IHVR-17028 对 BVDV、TCRV 和 DENV 具有抑制作用， EC50 分别为0.4 μM、0.26 μM 和0.3 μM。IHVR-17028 可用于研究传染病。

IHVR-19029 is an effective endoplasmic reticulum (ER) α-glucosidases I and II inhibitor (IC50: 0.48 μM for ER a-glucosidase I). IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Ebola virus, Dengue virus, and Rift

IHVR-11029 is a potent inhibitor of ER α-glucosidase. IHVR-11029 is active against multiple hemorrhagic fever viruses and efficiently disrupts the morphogenesis of a broad spectrum of enveloped viruses.

Itacnosertib (TP-0184)是一种可口服的ACRV1 (ALK-2)、FLT3和JAK2抑制剂，能够抑制过表达ALK-2的肿瘤细胞生长，能够克服FLT3抑制剂耐药并与venetoclax协同抑制AML生长，具有潜在的抗肿瘤和抗白血病活性。

OD36 hydrochloride (OD-36 hydrochloride) 是一种强效的 RIPK2 抑制剂，IC50 为 5.3 nM。OD36 hydrochloride 是一种大环抑制剂，可与 ALK2 激酶 ATP 口袋有效结合，能有效拮抗突变 ALK2 信号传导和成骨分化。OD36 hydrochloride 靶向作用于 ALK2，KD 为 37 nM。

LDN193189 Tetrahydrochloride 是 BMPI 型受体的选择性抑制剂，能够抑制 ALK2 (IC50: 5 nM) 和 ALK3 (IC50: 30 nM)，对 ALK4，ALK5 和 ALK7 的作用效果弱 (IC50≥500 nM)。

Hypericin (Cyclosan) 属于天然蒽醌类化合物，是贯叶连翘的提取物，可以抑制 PKC、MAO、多巴胺-beta-羟化酶、逆转录酶、端粒酶和 CYP等。Hypericin 具有抗菌、抗病毒、抗肿瘤和抗抑郁活性。

Arvanil (N-Vanillylarachidonamide) 是一种合成辣椒素-安非他命杂交体，也是香草素受体1 (VR1) 和大麻素 1 (CB1)的配体，具有神经保护活性，抑制痉挛，通过在体内诱导 HCC 细胞铁死亡来增强顺铂化疗敏感性，通过与 MICU1 结合诱导肝细胞癌的铁死亡。

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。

TRPV1 (VR1) receptor antagonist

TRPV1 (VR1) vanilloid receptor partial agonist

vanilloid TRPV1 (VR1) receptor agonist

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.

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.

DD-161515 is a VR1 antagonist.

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。

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。

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。

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.

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