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Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha 7 selectivity


Reference:

Karig, G., Large, J. M., Sharples, C. G. V., Sutherland, A., Gallagher, T. and Wonnacott, S., 2003. Synthesis and nicotinic binding of novel phenyl derivatives of UB-165. Identifying factors associated with alpha 7 selectivity. Bioorganic & Medicinal Chemistry Letters, 13 (17), pp. 2825-2828.

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Official URL:

http://dx.doi.org/10.1016/s0960-894x(03)00594-8

Abstract

Four racemic phenyl-substituted analogues 3-6 of the potent nicotinic agonist UB-165 1 have been synthesised and evaluated against the alpha(4)beta(2), alpha(3)beta(4), and alpha(7) neuronal nicotinic receptors. The 2'-phenyl derivative 3 shows no activity at these major receptor subtypes. while the 4'-phenyl analogue 4 shows an enhanced level Of a7 selectivity as compared to UB-165 and deschloro UB-165 2. These results are discussed within the context of recent pharmacophore models.

Details

Item Type Articles
CreatorsKarig, G., Large, J. M., Sharples, C. G. V., Sutherland, A., Gallagher, T. and Wonnacott, S.
DOI10.1016/s0960-894x(03)00594-8
DepartmentsFaculty of Science > Biology & Biochemistry
RefereedYes
StatusPublished
ID Code4083

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