2. Academic Validation
  3. Indole-2-carboxamides as allosteric modulators of the cannabinoid CB₁ receptor

Indole-2-carboxamides as allosteric modulators of the cannabinoid CB₁ receptor

  • J Med Chem. 2012 Jun 14;55(11):5627-31. doi: 10.1021/jm201485c.
Francesco Piscitelli 1,  Alessia Ligresti,  Giuseppe La Regina,  Antonio Coluccia,  Ludovica Morera,  Marco Allarà,  Ettore Novellino,  Vincenzo Di Marzo,  Romano Silvestri
Affiliations

Affiliation

  • 1 Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
PMID: 22571451 DOI: 10.1021/jm201485c
Abstract

We synthesized new N-phenylethyl-1H-indole-2-carboxamides as the first SAR study of allosteric modulators of the CB(1) receptor. The presence of the carboxamide functionality was required in order to obtain a stimulatory effect. The maximum stimulatory activity on CB(1) was exerted by carboxamides 13 (EC(50) = 50 nM) and 21 (EC(50) = 90 nM) bearing a dimethylamino or piperidinyl group, respectively, at position 4 of the phenethyl moiety and a chlorine atom at position 5 of the indole.

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