AM-251 (drug)

AM-251
Identifiers
	IUPAC name 1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(1-piperidyl)pyrazole-3-carboxamide;
JSmol)	Interactive image;
	SMILES O=C(NN1CCCCC1)c4nn(c2ccc(Cl)cc2Cl)c(c3ccc(I)cc3)c4C;
	InChI InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) ; Key:BUZAJRPLUGXRAB-UHFFFAOYSA-N ;
	(verify)

AM-251 is an

CB₁ receptor (with a K_i value of 7.5 nM) than rimonabant, which has a K_i value of 11.5 nM, AM-251 is, however, about two-fold more selective for the CB₁ receptor when compared to rimonabant.^[1] Like rimonabant, it is additionally a μ-opioid receptor antagonist^[2] that attenuates analgesic effects.^[3]

AM251 has shown an

colon cancer cells.^[4]

See also

Discovery and development of Cannabinoid Receptor 1 Antagonists

References

PMID 10052983
.

PMID 22771770
.

PMID 22771770
.

S2CID 205526223. Archived
(PDF) from the original on July 2, 2021.

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Retrieved from "https://en.wikipedia.org/w/index.php?title=AM-251_(drug)&oldid=1203337425"

[1] PMID 10052983
.

[2] PMID 22771770
.

[3] PMID 22771770
.

[4] S2CID 205526223. Archived
(PDF) from the original on July 2, 2021.

[1]

[2]

[3]

[4]