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  • Title: 1,2,5-Thiadiazole derivatives of arecoline stimulate M1 receptors coupled to phosphoinositide turnover.
    Author: Periyasamy S, Messer WS, Roknich S, Sauerberg P, Hoss W.
    Journal: Brain Res; 1995 Sep 25; 693(1-2):118-23. PubMed ID: 8653399.
    Abstract:
    A series of alkoxy-1,2,5-thiadiazole derivatives of arecoline was synthesized in an effort to develop M1 muscarinic agonists. The 3-butenyloxy, 2-butynyloxy, cyclopropylmethyloxy, and hexyloxy derivatives stimulated phosphoinositide turnover through muscarinic receptors in the rat hippocampus. The dose-response curves of 2-butynyloxy, cyclopropylmethyloxy and hexyloxy compound together was the same as the response of each separately. Pirenzepine was somewhat more potent than AF-DX 116 for inhibiting the responses produced by low concentrations of thiadiazole derivatives. The data suggest that the cyclopropylmethyloxy-TZTP derivative is functionally a selective M1 agonist. Molecular mechanics calculations indicate that the anti form of the 1,2,5-thiadiazole derivatives of arecoline may be active at M1 receptors.
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