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MDMB-4en-PINACA[3] (also incorrectly call 5-CL-ADB-A) is an indazole-base synthetic cannabinoid that sells online as a designer drug.] MDMB-4en-PINACA first in Europe in 2017.[10] In 2021, MDMB-4en-PINACA was the most common synthetic cannabinoid identify by the Drug Enforcement Administration in the US.[11] MDMB-4en-PINACA differs from 5F-MDMB-PINACA due to replacement of 5-fluoropentyl with a pent-4-ene moiety (4-en).[12]
Etymology
MDMB-4en-PINACA partially follows the cannabinoid naming scheme of LinkedGroup–TailChain–Core–Linker,[13] where:
- MDMB stands for Methyl DiMethyl Butanoate, the linked group.
- 4en stands for 4–en-1-yl, part of the carbon chain.
- PINACA stands for Pentyl-1H-INdAzole-3-CarboxAmide, the core group and linker.
Pharmacology
It acts as a potent agonist of the CB1 receptor with an EC50 value of 2.47 nM.
[14][15][16][17] MDMB-4en-PINACA reports to be approximately 2.5x to 3x+ (2.47 nM, 239%) stronger (by CB1 activate β-
arrestin 2 recruitment) than JWH-018 (25.3 nM, 100%) with over 10x the binding affinity than JWH-018 in vitro.[18]
In a review of in vitro MDMB-4en-PINACA studies shows an EC50 of 1.
, an Emax of 221–299% (compares to JWH-018), and a Ki value of 0.
28nM on the CB1 receptor[19]Â Â and appears
to be 7x more selective for the CB2 receptor over the CB1 receptor.
[20]Â MDMB-4en-PINACA has an in vitro half-life of approximately 10 minutes[21]
but has reportes in human urine samples
up to an hour after consumption, producing 14 metabolites which may have their own pharmacological activity and be use in
identification of MDMB-4en-PINACA consumption.[22]
