Drug intelligence / Profile preview

arachidonyl-2-chloroethylamide

Development stage
Preclinical
Modality
Small Molecules
Administration
Experimental (primarily Intraperitoneal In Animal Studies)
01

Overview

**Arachidonyl-2-chloroethylamide (ACEA)** is a synthetic, highly potent, and selective agonist of the cannabinoid type 1 (**CB1**) receptor, with a subnanomolar inhibitory constant (Ki = 1.4 nM for CB1) and much lower affinity for CB2 (Ki > 2000 nM)[1][2][4][6]. It is a structural analog of anandamide (AEA) and is used extensively in research settings to probe the function of the endocannabinoid system. Mechanistically, ACEA mimics the effects of endogenous cannabinoids by selectively activating CB1 receptors, leading to effects such as hypothermia and neuroprotection in animal models[6][7]. It is rapidly metabolized by fatty acid amide hydrolase (FAAH), which limits its in vivo duration of action unless FAAH is pharmacologically inhibited[7]. ACEA is not approved for clinical use and is distributed strictly for scientific research purposes.

Other names
(5Z,8Z,11Z,14Z)-N-(2-chloroethyl)icosa-5,8,11,14-tetraenamidearachidonyl-2'-chloroethylamide
02

Targets

CNR1 (Cannabinoid receptor 1)

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