Structure‐activity studies on the potentiation of benzodiazepine receptor binding by ethylenediamine analogues and derivatives

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Abstract
The effect of ethylenediamine analogues on in vitro binding of [3H]‐diazepam to crude cerebral cortical synaptosomal membranes in the rat was studied. Ethylenediamine significantly increased [3H]‐diazepam binding to a maximum potentiation of 154% control (EC50 = 18 × 10−4 M) and was the most active compound studied in terms of both potency and the maximum potentiation observed. Potentiation of [3H]‐diazepam binding by ethylenediamine analogues is dependent on carbon‐chain length, appears to require two terminal amino groups, and is not observed in the rigid analogues studied. Potentiation of [3H]‐diazepam binding by ethylenediamine analogues is mediated largely by a change in receptor number and not receptor affinity. Results are discussed in terms of the possible nature of the ethylenediamine binding site.