anandamide

Anandamide ((5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide) 是一种免疫调节剂，通过大麻素受体 CB1 和 CB2 起作用，还通过中枢神经系统中的其他靶点起作用，如 GPR18 GPR55。

LY2183240 是大麻素摄取阻滞剂。它是内源性大麻素降解酶脂肪酸酰胺水解酶的有效共价抑制剂。它抑制脂肪酸酰胺水解酶 (FAAH) 活性，IC50 为12.4 nM。它也抑制其他几种脑丝氨酸水解酶，对 MAG 脂肪酶、bh6 和 KIAA1363 的 IC50分别为 5.3、0.09 和 8.2 nM。

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。

OMDM-6 是 TRPV1(EC50 = 75 nM) 和 CB1 (Ki = 3.2 μM) 的双重激动剂。 OMDM-6 抑制 anandamide 细胞摄取，Ki 为 7.0 μM。

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)。

BI-0314 is a selective allosteric STEP activator.

BIA 10-2474 是一种长效可逆的脂肪酸酰胺水解酶抑制剂，与人类内源性大麻素系统相互作用，可增加中枢神经系统和外周组织，对大鼠大脑不同区域的 IC50值为50至70mg kg。它用于治疗焦虑症、帕金森氏病和多发性硬化症、高血压或肥胖症的慢性疼痛。

ARN272 是大麻素转运抑制剂的一种。

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。

OMDM-2 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 3.0 μM).

OMDM-3 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 16.6 μM).

OMDM-4 is a selective and metabolically stable anandamide cellular uptake (ACU)inhibitor(Ki of 17.7 μM).

MAFP (Methyl Arachidonyl Fluorophosphonate) 是选择性，针对活性位点，不可逆的 cPLA2 和 iPLA2 抑制剂。 MAFP 也是一种有效的不可逆的 anandamide amidase 抑制剂。

ASP8477是一种高效且选择性的FAAH抑制剂。该化合物通过口服活性能增加大脑中的阿纳米酰胺（anandamide）水平。在大鼠的神经病理性及骨关节炎疼痛模型中，ASP8477显示出良好的疗效，且不引起运动协调障碍。单次口服ASP8477能改善慢性压迫性神经损伤大鼠的热性痛觉过敏和寒冷痛觉异常。此外，ASP8477还能恢复由利血平引起的肌肉压力阈值下降的肌痛大鼠模型。研究表明，ASP8477在缓解神经病理性和功能性疼痛方面具有镇痛效果，其药理特性适合用于治疗慢性疼痛。

N-Stearoyltyrosine (N-(1-Oxooctadecyl)-L-tyrosine) 是 Anandamide 的类似物。在沙鼠缺血再灌注模型中，N-Stearoyltyrosine 通过保护海马体 CA1 区显示出神经保护作用，并能抑制自由基的产生以及提高抗氧化能力。该化合物还可抑制 IR 诱导的细胞凋亡 (apoptosis)。

biotinylated anandamide analog acts as a probe for visualizing the accumulation and intracellular trafficking of anandamide

anandamide uptake inhibitor

anandamide transport inhibitor

The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 μg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 μM).

N-Acylated ethanolamines (NAE) are naturally-occurring lipids that have diverse bioactivities. The different types of NAE can be derived from glycerophospho-linked precursors by the activity of glycerophosphodiesterase 1 (GDE1). Glycerophospho-N-arachidonoyl ethanolamine is the precursor of arachidonoyl ethanolamide (AEA), also known as anandamide. AEA is an endogenous cannabinoid neurotransmitter that binds to both central cannabinoid (CB1) and peripheral cannabinoid (CB2) receptors. It inhibits the specific binding of [3H]-HU-243 to synaptosomal membranes with a Ki value of 52 nM, compared to 46 nM for δ9-THC.

Anandamide (arachidonoyl ethanolamide; AEA) is an endogenous lipid with cannabinergic activity; along with 2-arachidonoyl glycerol, it forms part of the endocannabinoid system. AEA undergoes reuptake into neurons by a facilitated process. Controversy exists as to whether there is a specific AEA transporter, or instead the uptake process is simply driven by hydrolysis of AEA by intracellular fatty acyl amide hydrolase (FAAH). CAY10412 is an analog of AEA that has no intrinsic binding affinity for either CB1 or CB2 receptors. It is a potent inhibitor of AEA reuptake in U937 lymphoma cells, with an IC50 of 3 μM. CAY10412 could be a useful tool for distinguishing the competing transporter theories. The pharmacology of CAY10412 is largely unexplored; it may enhance endocannabinoid signalling by augmenting endocannabinoid concentrations.

Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids.

Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of miniature inhibitory postsynaptic currents in primary cultured hippocampal neurons, an effect which is the opposite of that induced by anandamide.. PGD2-EA also induces apoptosis in colorectal carcinoma cell lines.

AM404 是一种内源性大麻素再摄取抑制剂，是 TRPV（1） 激活剂，是扑热息痛代谢物，具有神经保护作用和抗癌活性，可阻断 anandamide 转运。AM404 抑制 NFAT 和 NF-kappaB 信号通路，并损害神经母细胞瘤细胞的迁移和侵袭性，通过抑制 COX 活性来阻止活化的小胶质细胞中前列腺素的合成。