Thyroid hormones and derivatives inhibit flunitrazepam binding.

A Nagy; A Lajtha

doi:10.1111/j.1471-4159.1983.tb11298.x

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Thyroid hormones and derivatives inhibit flunitrazepam binding.

A Nagy·A Lajtha

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Abstract

Thyroid hormones and their derivatives were found to inhibit [3H]flunitrazepam binding stereospecifically and in a monophasic manner. Among the compounds tested, D-thyroxine was the most potent inhibitor (IC50 = 0.5 microM). The naturally occurring L-thyroxine was about 40-fold less potent (IC50 = 20 microM). The structure-activity relationships seem to imply that the thyronine base has the principal role in the inhibition of benzodiazepine receptor binding. The type of inhibition was examined with the most potent inhibitor, D-thyroxine, by Scatchard analysis. The apparent dissociation constant (KD) of the [3H]flunitrazepam binding increased and the receptor density (Bmax) decreased as a function of D-thyroxine concentration; this is characteristic of mixed-type inhibition.

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Animals Anti-Anxiety Agents Brain Flunitrazepam Kinetics Mice Receptors, Cell Surface Receptors, GABA-A Stereoisomerism Structure-Activity Relationship Thyroid Hormones Thyroxine Triiodothyronine Journal Article

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A Nagy, A Lajtha. 1983. Thyroid hormones and derivatives inhibit flunitrazepam binding.. https://doi.org/10.1111/j.1471-4159.1983.tb11298.x

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