Abstract
Few agents (agonists) bind at [3H]nicotine-labeled nicotine receptors with an affinity comparable to that of nicotine. We initially approached this problem by undertaking a systematic structure-affinity study to determine the contribution to binding of various aspects of the nicotine molecule and of nicotine-related derivatives. For example a series of aryl-substituted and unsubstituted, primary, secondary, and tertiary amine derivatives of 3-(aminomethyl)pyridine (1) were prepared and examined. The finding that 1 (R = Me, R’ = Et, X = H) binds with good affinity (Ki = 28 nM) led to the synthesis of several conformationally-restricted analogs, such as 2 and 3 (Ki = 85 and 12 nM, respectively). With the availability of such structure-affinity and conformational data, it should now be possible to optimize affintiy by design and synthesis of new compounds. (Supported in part by funding from TDC/CIT.)
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© 1994 Springer Basel AG
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Fiedler, W. et al. (1994). Novel nicotinic receptor ligands. In: Clarke, P.B.S., Quik, M., Thurau, K., Adlkofer, F. (eds) International Symposium on Nicotine: The Effects of Nicotine on Biological Systems II. Experientia Supplementum, vol 71. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-7416-8_9
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DOI: https://doi.org/10.1007/978-3-0348-7416-8_9
Publisher Name: Birkhäuser, Basel
Print ISBN: 978-3-7643-5087-1
Online ISBN: 978-3-0348-7416-8
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