The pharmacological profile of the competitive muscarinic antagonist (2S, 3'R) 3-quinuclidinyl tropate, abbreviated (-)-2a, was evaluated on rabbit vas deferens (M1/M4-like; pA2=9.10), guinea-pig left atrium (M2; pA2=9.30), guinea-pig ileum (M3; pA2=10.33) and guinea-pig uterus (M4 putative; pA2=9.70) muscarinic receptors and on the five subtypes of muscarinic receptors expressed individually in CHO-K1 cells. The drug shows an affinity for the M3 receptor subtype at least 10-fold higher than 4-DAMP, p-HHSiD and zamifenacin, used as reference drugs. These results suggest (-)-2a as a novel, potent and selective M3 antagonist that may have therapeutic potential in the treatment of conditions associated with increased smooth muscle contractility

In vitro characterization of a novel, potent and selective M3 antagonist / C. GHELARDINI; A. BARTOLINI; N. GALEOTTI; C. BELLUCCI; S. DEI; F. GUALTIERI. - In: LIFE SCIENCES. - ISSN 0024-3205. - STAMPA. - 61:(1997), pp. 1217-1226. [10.1016/S0024-3205(97)00666-8]

In vitro characterization of a novel, potent and selective M3 antagonist

GHELARDINI, CARLA;BARTOLINI, ALESSANDRO;GALEOTTI, NICOLETTA;BELLUCCI, CRISTINA;DEI, SILVIA;GUALTIERI, FULVIO
1997

Abstract

The pharmacological profile of the competitive muscarinic antagonist (2S, 3'R) 3-quinuclidinyl tropate, abbreviated (-)-2a, was evaluated on rabbit vas deferens (M1/M4-like; pA2=9.10), guinea-pig left atrium (M2; pA2=9.30), guinea-pig ileum (M3; pA2=10.33) and guinea-pig uterus (M4 putative; pA2=9.70) muscarinic receptors and on the five subtypes of muscarinic receptors expressed individually in CHO-K1 cells. The drug shows an affinity for the M3 receptor subtype at least 10-fold higher than 4-DAMP, p-HHSiD and zamifenacin, used as reference drugs. These results suggest (-)-2a as a novel, potent and selective M3 antagonist that may have therapeutic potential in the treatment of conditions associated with increased smooth muscle contractility
1997
61
1217
1226
C. GHELARDINI; A. BARTOLINI; N. GALEOTTI; C. BELLUCCI; S. DEI; F. GUALTIERI
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/310662
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