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R J Breckenridge

Publications and source records attributed to R J Breckenridge.

5 recordsLinked to original sources

Molecular recognition: models for drug design.

The review takes examples, mostly from the recent literature, to illustrate how an understanding of physico-chemical properties and an appreciation of the molecular shape and electronic properties can lead to a better insight into molecular recognition processes. The techniques used to generate 3-dimensional structures of molecules and the influence this information has had on the drug design cycle, are briefly discussed.

Amino Acid Sequence↗

Inhibition of [3H]GABA binding to postsynaptic receptors in human cerebellar synaptic membranes by carboxyl and amino derivatives of GABA.

Fifty synthetic analogues of GABA were tested for their ability ot interact with GABA receptors, using [3H]GABA binding to human cerebellar membranes as an in vitro model. The most active compounds were found to be aliphatic and heterocyclic aminosulphonic acids. Compounds with highly substituted nitrogen atoms were only weakly active unless a long alkyl chain, which can interact with the postsynaptic membrane, was present. It was concluded that a pyramidal nitrogen atom is favoured fro binding of GABA analogues to human cerebellar membranes.

Cerebellum↗