794572-10-4

CID2440433, also known as ML-184, is a potent synthetic agonist of GPR55 (EC50 = 0.26 μM). GPR55 is a G protein-coupled receptor that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 μM lysophosphatidylinositol (LPI).

ML-184 (CID2440433) is a selective GPR55 agonist with an EC50 of 250 nM and exhibits >100-fold selectivity for GPR55 over GPR35, CB1?and CB2. ML-184 induces phosphorylation of ERK1/2 and translocation of PKCβII to the plasma membrane by activating GPR55[1]. ML-184(CID2440433) increases proliferation of neural stem cells and promotes neuronal differentiation?in vitro[2].

ChEBI: 3-[[4-(2,3-dimethylphenyl)-1-piperazinyl]-oxomethyl]-N,N-dimethyl-4-(1-pyrrolidinyl)benzenesulfonamide is a member of piperazines.

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[1] Kotsikorou E, et al. Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2011 Jun 28;50(25):5633-47. DOI:10.1021/bi200010k
[2] Hill JD, et al. Activation of GPR55 increases neural stem cell proliferation and promotes early adult hippocampal neurogenesis. Br J Pharmacol. 2018 Aug;175(16):3407-3421. DOI:10.1111/bph.14387