cb-1-in-1

CB1-IN-1 (DBPR211) 是新型的外周大麻素-1受体 (CB1R) 拮抗剂，作用于CB1R (EC50 = 3 nM) 和 CB2R 的Ki 分别为0.3 nM 和 21 nM。

ABCB1-IN-1 (compound 3) 为高效ABCB1抑制剂，可诱导细胞凋亡。含1-苯甲基咪唑基团，其对Colo205与Colo320细胞系展现出的IC50分别为1.26 μM与2.21 μM。

CB-6644 是CB-6644是RUVBL1 2复合物ATP酶活性的变抗小分子抑制剂，在癌细胞中特异性地与RUVBL1 2相互作用，阻断RUVBL1 2的ATPase活性，其半数最大抑制浓度（IC50）为15 nM[1]。

COR659 是一种有效的 GABAB 的阳性变构调节剂。COR659具有缓解大鼠对酒精和巧克力成瘾的作用。

CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).

O-2050 是一种高亲和力的大麻素CB1受体拮抗剂，Ki 为 2.5 nM。O-2050 抑制大麻素 CB2受体，Ki 为 0.2 nM。O-2050 减少了小鼠的食物摄入量，并且引起小鼠运动。

OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microMing activities in

AZD1940 (UNII-0J0035E9FT)是一种高亲和力的大麻素CB(1) CB(2)受体激动剂，具有口服活性，应用于口面疼痛的研究。

N-Acyl ethanolamines (NAEs) have diverse biological actions that are strongly affected by the associated acyl group. Docosahexaenoyl ethanolamide (DHEA) has potential signaling roles in cancer, inflammation, and neurological development and functioning. At least some of DHEA's effects are mediated through cannabinoid (CB) receptors, while some NAEs also act as vanilloid receptor agonists and voltage-gated K+ channel blockers. (R)-(+)-Docosahexaenyl-1'-hydroxy-2'-propylamide is a homolog of DHEA, characterized by the addition of an (R)-α-methyl group at the methylene carbon adjacent to the amide nitrogen. A similar modification of arachidonoyl ethanolamide to produce R-1 methanandamide imparts higher affinity for the CB receptor as well as improved metabolic stability. The physiological actions of this compound have not been evaluated.

Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1 2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.

(±)-Ibipinabant ((±)-SLV319) 是一种有效选择性的大麻素-1 (CB-1) 受体拮抗剂，IC50=22 nM。(±)-SLV319 是 SLV319的消旋体。

Linderalactone 是从乌药中分离出来的一种倍半萜烯内酯，通过调节凋亡相关蛋白的表达和抑制 JAK STAT 信号通路来抑制癌细胞生长。它以 IC50值为 15 µM 来抑制肺癌 A-549 细胞的增殖。

CB-25是一种CB1大麻素受体的部分激动剂配体。它能增强Forskolin诱导的癌细胞中cAMP的形成，但在Forskolin诱导的hCB1-CHO细胞中则不显示增强作用。

Linoleoyl ethanolamide 是脂肪酸乙醇酰胺。它可弱结合 CB1 和 CB2 受体，并分别抑制[3H]CP-55,940的结合，Ki 分别为 10 和 25μM。它在引起小鼠过氧化氢酶方面的效力是 anandamide 的4倍，且对睡眠时间无延长效果。