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  • Title: Quinuclidin-2-ene-based muscarinic antagonists.
    Author: Hacksell U, Nilsson BM, Nordvall G, Johansson G, Sundquist S, Nilvebrant L.
    Journal: Life Sci; 1995; 56(11-12):831-6. PubMed ID: 10188782.
    Abstract:
    A series of achiral 3-heteroaryl substituted quinuclidin-2-ene derivatives and related compounds have been synthesized by facile methods. The compounds were evaluated for muscarinic and antimuscarinic properties in receptor binding studies using (-)-[3H]-QNB as the radioligand and in a functional assay using isolated guinea pig urinary bladder. 3-(2-Benzofuranyl)-quinuclidin-2-ene (15) displayed the highest M1-receptor affinity in the present series (Ki = 9.6 nM).
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