title: 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: an effective scaffold for the design of either CB1 or CB2 receptor ligands.
abstract: New 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized as cannabinoid (CB) receptor ligands. Compound 11 (CB(1)K(i) = 2.3 nM, CB(1) SI = 163.6) showed CB(1) receptor affinity and selectivity superior to Rimonabant and AM251. Acute administration of 2mg/kg 11 reduced sucrose, but not regular food, intake in rats. On the other hand, compound 23 (CB(2)K(i) = 0.51 nM, CB(2) SI = 30.0) showed significant affinity and selectivity for the CB(2) 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 CB(1) or CB(2) receptor ligands.
authors: Istituto Pasteur - Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
authors: Francesco
authors: F
authors: Piscitelli
authors: Alessia
authors: A
authors: Ligresti
authors: Giuseppe
authors: G
authors: La Regina
authors: Valerio
authors: V
authors: Gatti
authors: Antonella
authors: A
authors: Brizzi
authors: Serena
authors: S
authors: Pasquini
authors: Marco
authors: M
authors: Allarà
authors: Mauro Antonio Maria
authors: MA
authors: Carai
authors: Ettore
authors: E
authors: Novellino
authors: Giancarlo
authors: G
authors: Colombo
authors: Vincenzo
authors: V
authors: Di Marzo
authors: Federico
authors: F
authors: Corelli
authors: Romano
authors: R
authors: Silvestri
mesh_terms: D000818:Animals; D015195:Drug Design; D004435:Eating / Q000187:drug effects; D006801:Humans; D008024:Ligands; D008297:Male; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D043884:Receptor, Cannabinoid, CB1 / Q000378:metabolism*; D043885:Receptor, Cannabinoid, CB2 / Q000378:metabolism*; D013379:Substrate Specificity
chemical_list: D008024:Ligands; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D043885:Receptor, Cannabinoid, CB2