Comparative thermodynamics of benzodiazepine receptor ligand interactions in rat neuronal membranes.

Abstract:

:The effects of temperature on the interaction of various ligands with the benzodiazepine receptor were studied in rat brain membrane preparations. The affinities of all ligands studied were reduced on raising the temperature from 4 to 37 degrees C. The variation of affinity constant with temperature deviated from the classical relationship for both the anticonvulsant ligand [3H]flunitrazepam and the proconvulsant ligand [3H]ethyl beta-carboline-3-carboxylate. This implies a variation of observed enthalpy change of binding with temperature. Possible reasons for this are discussed. Gamma-Aminobutyric acid and sodium chloride both enhance the binding of [3H]flunitrazepam--the former by an increase in the entropic component of the binding energy, and the latter by an increase in the enthalpic component. In a series of ligands of different biological activities, no simple correlation was observed between biological activity and temperature dependence of binding.

journal_name

J Neurochem

authors

Doble A

doi

10.1111/j.1471-4159.1983.tb08133.x

subject

Has Abstract

pub_date

1983-06-01 00:00:00

pages

1605-12

issue

6

eissn

0022-3042

issn

1471-4159

journal_volume

40

pub_type

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