Abstract
Several heterocyclic N-piperidine substituted salts were synthesized that were found to inhibit the specific binding of the antagonist [3H] quinuclidinyl benzilate in radioligand muscarinic binding assays (3H-QNB) in bioassays. One of the heterocyclic salts, compound 7, met the significance criteria in these assays (>50% inhibition) at 10 μM of the nonselective muscarinic antagonist (3H-QNB) in cells of the Wistar rat cerebral cortex. Furthermore, this compound displayed 61% inhibition at 10 μM of the antagonist (3H-QNB) for the M5 receptor (IC50 6.34 μM, Ki 3.93 μM, nH = 0.996) in human recombinant CHO cell lines. These data obtained from Ricerca Biosciences suggested that compound 7 was selective for the M5 receptor. Another study from the Czech Academy of Sciences demonstrated that compound 7 was 3 to 8 times more potent at M2 than other subtypes of muscarinic receptors in competition with antagonist N-methylscopolamine and selective for the M1 receptors over M3 and M5 in antagonizing accumulation of inositol phosphates induced by muscarinic agonist carbachol.
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