1,720,985 research outputs found
. “Synthesis, Pharmacological “Evaluation and Selectivity Profile of Isomeric 2-Phenyl-2-Cyclohexyl-4-[(Dimethylamino)Methyl]-1,3-Dithiolane Methiodides, as Potent Antimuscarinic Agents”.
No full textSynthesis, Pharmacological Evaluation and Selectivity Profile of Isomeric 2-Phenyl-2-cyclohexyl-4-[(dimethylamino)methyl]-1,3-dithiolane Methiodide as Potent Antimuscarinic Agents
No full textThe synthesis and antimuscarinic activity on M1, M 2 and M3 tissues of cis- and trans-2-phenyl-2-cyclohexyl-4-[(dimethylamino)-methyl]-1,3-dithiolane methiodides (1 and 2)are described. Our results show that compound 1 is a potent and Mr1 selective muscarinic antagonist
Determination of Muscarinic Agonist Potencies at M1 and M2 Receptors in Pithed Rat
No full textThe agonist potency of 2-cia-methyl-5-dimethylaminomethyl-1,3-oxathiolane-3-traqns-oxide methiodide and its two enantiomers were detemined in vivo at muscarinic M1 and M2 receptors. The results indicate a selectivity of 5-8 fold for M1 receptors, confirming the M1 profile of the oxathiolane nucleus
Synthesis and alpha-blocking activity of some analogues of idazoxan
No full textSeveral analogues of idazoxan 1 and fenmetazole 2 were prepared as potential alpha2-adrenoreceptor antagonists. Their blocking activity and selectivity on alpha1- and alpha2-adrenoreceptors were evaluated in isolated rat vas deferens. Although all the drugs displayed a significantly lower activity compared to the parent compounds 1 and 2, with 3 being the only exception, the present results might help in elucidating the role of ring oxygens of 1 in drug—receptor interaction
“Synthesis, “NMR Spectroscopy Study, and Antimuscarinic Activity of a Series of 2-(Acyloxymethyl)-1,3-dioxolane”.
No full textResolution of the potent alpha1-adrenoreceptor antagonist 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzoxathian (benoxathian)
No full textThe enantiomers of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]methyl]-1,4-benzoxathian hydrochloride (1: benoxathian) were prepared from the chiral 1,4-benzoxathian-2-carboxylic acids [(+)- and (−)-3] which in turn were obtained through the resolution of the racemic acid with R- and S-alpha-methylbenzylamine. Their blocking activities and relative selectivities on alpha1- and alpha2-adrenoreceptors were evaluated on isolated rat vas deferens. For alpha1-adrenoreceptors the enantiomer (−)-1 was 10 times more potent than the enantiomer (+)-1, whereas no significant difference between the blocking activity of the enantiomers was observed for alpha2-adrenoreceptors. Furthermore, the enantiomer (−)-1 showed high activity and selectivity toward the alpha1-adrenoreceptor (pA2 = 9.36; selectivity ratio = 1230) which may have relevance in the characterization of alpha-adrenoreceptor subtypes
“Synthesis and α1-Antagonist Activity of New Prazosin-and Benextramine-Related Tetraamine Disulfides”.
No full textSynthesis and antimuscarinic activity of derivatives of 2-substituted-1,3-dioxolanes
No full textGeometric cis, trans isomers, derivatives of 2-substituted-1,3-dioxolanes and 2-substituted-1,3-dioxanes were designed and studied as antimuscarinic agents. The synthesized compounds were evaluated as perchlorides and methiodides by functional tests with rabit vas deferens (putatvie M1), guinea-pig heart (M2) and guinea-pig ileum (M3). The effect of the replacement of a trimethylammonium group with a dimethylsulfonium in the two rings was also evalutated. Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptorsGeometric cis, traits isomers, derivatives of 2-substituted-1,3-dioxolanes and 2-substituted-1,3-dioxanes were designed and studied as antimuscarinic agents. The synthesized compounds were evaluated as perchlorides and methiodides by functional tests with rabbit vas deferens (putative M-1), guinea-pig heart (M-2) and guinea-pig ileum (M-3). The effect of the replacement of a trimethylammonium group with a dimethylsulfonium in the two rings was also evaluated. Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptors
Studio farmacologico del (+)-cyclazosin, un antagonista selettivo del recettore alfa 1B-adrenergico
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