| Title : S-(-)-ET 126: a potent and selective M1 antagonist in vitro and in vivo - Ghelardini_1996_Life.Sci_58_991 |
| Author(s) : Ghelardini C , Bartolini A , Galeotti N , Teodori E , Gualtieri F |
| Ref : Life Sciences , 58 :991 , 1996 |
|
Abstract :
The pharmacological profile of the competitive muscarinic antagonist S-(-)-alpha-(hydroxymethyl)benzeneacetic acid 1-methyl-4-piperidinyl ester (S-(-)-ET 126) was evaluated on M1 (rabbit vas deferens; pA2=8.99), M2 (rat left atrium; pA2=8.21) and M3 (rat ileum; pA2=6.84) muscarinic receptors in comparison with pirenzepine. The drug shows a subtype selectivity (M1/M2=8; M1/M3=178; M2/M3=22) that proposes it as a useful pharmacological tool for receptor studies. S-(-)-ET 126, like pirenzepine, prevents the antinociception induced by M1 agonists (McN-A-343 and AF-102B). Unlike pirenzepine and spirotramine, the compound is able to cross the blood brain barrier which makes it useful for in vivo investigations. |
| PubMedSearch : Ghelardini_1996_Life.Sci_58_991 |
| PubMedID: 8786711 |
Ghelardini C, Bartolini A, Galeotti N, Teodori E, Gualtieri F (1996)
S-(-)-ET 126: a potent and selective M1 antagonist in vitro and in vivo
Life Sciences
58 :991
Ghelardini C, Bartolini A, Galeotti N, Teodori E, Gualtieri F (1996)
Life Sciences
58 :991