Massimo Nicola

Marco Turconi; Arturo Donetti; Antonio Schiavone; Angelo Sagrada; Ernesto Montagna; Massimo Nicola; Raffaele Cesana; Carlo A. Rizzi; Rosella Micheletti

The pharmacological profile of six representative members of a novel class of 5-HT3 receptor antagonists is described. The compounds are esters and amides of benzimidazolone-1-carboxylic acid with a basic azabicycloalkyl moiety (compounds 1-3) and their respective ethyl derivatives (compounds 4-6). In isolated preparations (rabbit heart and guinea pig ileum) all compounds antagonized the 5-HT3 receptor-mediated effects of serotonin, with potencies comparable with those of the reference compounds, ICS 205.930 and GR 38032F (-log IC50 9.30-11.9 and 6.8-8.20, in heart and ileum, respectively). In the anaesthetised rat, all agents potently inhibited the Bezold-Jarisch reflex whether given i.v. or i.d. I.v. administration of compounds prevented cisplatin-induced emesis in dogs (ID50 ranging from 3.7 to 147 micrograms/kg). All agents accelerated gastric emptying of solids in rats (ED50 about 10-160 micrograms/kg i.p.). In addition, compounds 4 and 5 were able to stimulate 5-HT4 receptors in the isolated guinea pig ileum, as well as enhance contractile activity in the Heidenhain gastric pouch of dogs, showing clearcut prokinetic properties.

Marco Turconi; Massimo Nicola; Myrna Gil Quintero; Luciano Maiocchi; Rosella Micheletti; Ettore Giraldo; Arturo Donetti

Marco Turconi; Arturo Donetti; Ernesto Montagna; Massimo Nicola; Annamaria Uberti; Rosamaria Micheletti; Antonio Giachetti

Marco Turconi; Arturo Donetti; Ernesto Montagna; Massimo Nicola; Annamaria Uberti; Rosamaria Micheletti; Antonio Giachetti

Arturo Donetti; Marco Turconi; Massimo Nicola; Rosamaria Micheletti

Arturo Donetti; Marco Turconi; Massimo Nicola; Rosamaria Micheletti

Massimo Nicola; Arturo Donetti; Enzo Cereda; Marco Turconi; Giovanni Battista Schiavi; Rosamaria Micheletti

Massimo Nicola; Arturo Donetti; Enzo Cereda; Marco Turconi; Giovanni Battista Schiavi; Rosamaria Micheletti

Arturo Donetti; Marco Turconi; Massimo Nicola; Rosamaria Micheletti

Arturo Donetti; Rosamaria Micheletti; Massimo Nicola; Marco Turconi