A novel analog of TRH, YM14673, causes a decrease in brain TRH receptors in vitro.

Abstract:

:Biochemical mechanisms by which analogs of thyrotropin-releasing hormone (TRH) produce their potent neuropharmacological actions on the brain remain ill-defined. We tested effects of YM14673, a novel analog of TRH, on TRH receptors in rat brains in vitro. No significant binding of [3H]YM14673 to brain plasma membranes occurred. In contrast, preincubation of membranes with YM14673 caused dose-dependent decreases in TRH binding. This was not due to competition for TRH binding sites or existence of metabolites of YM14673. Preincubation with DN1417 (an another TRH analog), cyclo(His-Pro) or methionine-enkephalin did not affect the binding. Affections of YM14673 on TRH binding were observed when cerebral cortical membranes were studied; those were not seen in membranes prepared from hypothalamus, striatum, midbrain, hippocampus, or pons-medulla. The present data indicate that YM14673 exerts its characteristic neuro-pharmacological functions through interacting with TRH binding sites in the brain.

journal_name

Endocr Res

journal_title

Endocrine research

authors

Monden T,Mizuma H,Yamada M,Murakami M,Mori M

doi

10.1080/07435809509030493

subject

Has Abstract

pub_date

1995-11-01 00:00:00

pages

803-14

issue

4

eissn

0743-5800

issn

1532-4206

journal_volume

21

pub_type

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