生物活性 | |||
---|---|---|---|
描述 | Muscarinic receptors have been tentatively subclassified to M1 and M2 on the basis of differences in their affinity for the cholinergic antagonist pirenzepine. 5'-isobutylthio-adenosine (SIBA) is best known as inhibitor of S-adenosylhomocysteine hydrolase, but has also been implicated as inhihitors of protein synthesis, nucleic acid synthesis, viral replication, cellular differentiation, chemotaxis, polyamine metabolism and IgE-mediated histamine release. Most of these effects have been attributed to the inhibition of transmethylation reactions. SIBA also has biological and biochemical effects over muscarinic receptors other than on transmethylation reactions. SIBA, at 100 µM, inhibited [3H]N-methyl-scopolamine binding to homogenates of whole brain and cortex (mainly M1 subtype receptors) by 11-30% and to cerebellum (mainly M2 subtype receptors) by 20-39%. At 0.01-1.0 µM, stimulation of [3H]QNB and NMS-inaccessible [3H]QNB binding was observed, with the most induced by 1 µM 3-deaza-SIBA. In contrast, [3H]pirenzepine ([3H]PZ) binding to whole brain and cortex was inhibited in a dose-dependent manner with Ki values in the µM range[3]. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.95mL 0.59mL 0.29mL |
14.73mL 2.95mL 1.47mL |
29.46mL 5.89mL 2.95mL |
参考文献 |
---|
[3]Muscarinic Receptor Subtype Specificity of 5'-(isobutylthio)-adenosine (SIBA) and Its Analogs |