AM251

AM251

Drugbox
IUPAC_name = 1-(2,4-dichlorophenyl)-5-(4-iodophenyl] )-4-methyl-
"N"-(1-piperidyl)pyrazole-3-carboxamide






width= 160
CAS_number= 183232-66-8
ATC_prefix=
ATC_suffix=
PubChem= 2125
DrugBank=
C=22 | H=21 | Cl=2 | I=1 | N=4 | O=1
molecular_weight =555.238 g/mol
bioavailability=
metabolism =
elimination_half-life=
excretion =
pregnancy_category =
legal_status =
routes_of_administration=

AM251 is a CB1 cannabinoid receptor antagonist. AM251 is structurally very close to SR141716A (rimonabant), which both are biarylpyrazole cannabinoid receptor antagonists. In AM251 the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group. The resulting compound exhibits slightly better binding affinity for the CB1 receptor with a Ki value of 7.5 nM compound to SR141716A, which has a Ki value of 11.5 nM. However AM251 is about two-fold more selective for the CB1 receptor when compared to SR141716A. [Lan, R., Liu, Q., Fan, P., et al. Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J Med Chem 42 769-776 (1999). PubMed|10052983]


References


Wikimedia Foundation. 2010.

Игры ⚽ Нужно сделать НИР?

Look at other dictionaries:

  • Cannabinoid receptor antagonist — The discovery of the endogenous cannabinoid system led to the development of CB1 receptor antagonists. The first cannabinoid receptor antagonist, rimonabant, was described in 1994. Rimonabant blocks the CB1 receptor selectively and it has been… …   Wikipedia

  • BML-190 — Drugbox IUPAC name = 2 [1 (4 chlorobenzoyl) 5 methoxy 2 methylindol 3 yl] 1 morpholin 4 ylethanone CAS number = ATC prefix = ATC suffix = PubChem = 2415 DrugBank = chemical formula = |C=23|H=23|Cl=1|N=2|O=4 molecular weight = 426.892 smiles =… …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”