1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: an effective scaffold for the design of either CB1 or CB2 receptor ligands.
- Piscitelli F.
- Ligresti A.
- La Regina G.
- Gatti V.
- Brizzi A.
- Pasquini S.
- Allarà M.
- Carai M.A.M.
- Novellino E.
- Colombo G.
- Di Marzo V.
- Corelli F.
- Silvestri R.
Publication date
January 2011
DOI Publisher
Elsevier BV ISSN
0223-5234 Citation count (estimate)
7Abstract
New 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized as cannabinoid (CB) receptor ligands. Compound 11 (CB1Ki = 2.3 nanoM, CB1 SI = 163.6) showed CB1 receptor affinity and selectivity superior to Rimonabant and AM251. Acute administration of 2 mg/kg 11 reduced sucrose, but not regular food, intake in rats. On the other hand, compound 23 (CB2Ki = 0.51 nanoM, CB2 SI = 30.0) showed significant affinity and selectivity for the CB2 receptor. The results presented here show that the 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide may serve as an effective scaffold for the design of either CB1 or CB2 receptor ligands
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