. beta.-Proline analogs as agonists at the strychnine-sensitive glycine receptor

G Johnson, JT Drummond, PA Boxer…

Index: Johnson, Graham; Drummond, James T.; Boxer, Peter A.; Bruns, Robert F. Journal of Medicinal Chemistry, 1992 , vol. 35, # 2 p. 233 - 241

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Citation Number: 15

Abstract

3-Carboxy-3, 4dehydropyrrolidine was found to bind with affinity equal to that of glycine in a [3H] strychnine binding assay. Simple substitution of the 1-, 2-, 4-, or 5-position resulted in marked loss of affinity. A decline in affinity was also found upon enlargement, contraction, or saturation of the &membered ring. However,@-proline and azetidine-3-carboxylic acid retained significant binding affinity. Despite its good affinity in [3H] strychnine binding, 3- ...