Low Affinity Analogs of Thyrotropin-releasing Hormone Are Super-agonists
نویسندگان
چکیده
منابع مشابه
Biological activities of thionated thyrotropin-releasing hormone analogs.
Analogs of thyrotropin-releasing hormone (Glp-His-Pro-NH2, TRH) have been prepared which contain thioamide moieties in the pyroglutamic acid ring, the carboxyamide proline terminus, and in both positions (dithio). These compounds have been tested for TSH-releasing activities (in vitro and in vivo), and for binding to TRH receptors in rat pituitary and cortex. The monothionated analogs showed no...
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Although the issue has not yet been fully resolved, there is reason to believe that TRI-I may have a trophic effect on the normal motoneuron and may transien tly improve the neurologic deficit in ALS. Since ALS is not a simple TRI-I deficiency disease, this improvement probably occurs via a secondary mecha -nism-possibly another neurotransmitter. It is uncertain at this time whether this effec...
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Endogenous thyrotropin-releasing hormone (TRH) reserve and pituitary thyrotropin (TSH) reserve were assessed in four normal subjects, three patients post-cryohypophysectomy, one patient with a hypothalamic lesion secondary to trauma, and four patients with Sheehan's syndrome. TSH reserve was determined by the immunoassayable TSH response to 500 mug TRH given i.v. (TRH stimulation test). TRH res...
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A time-dependent inhibition of the thyrotropin-releasing-hormone (TRH)-degrading ectoenzyme (EC 3.4.19.-) from rat brain by the metal-complexing agents imidazole, NaCN, EDTA and 1,10-phenanthroline could be demonstrated. In contrast, the inhibition by the non-chelating analogues 4,7and 1,7-phenanthroline was not time-dependent. At a concentration of 100 ,M EDTA the enzymic activity decreased by...
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Thyrotropin releasing hormone (TRH) and its receptors are present in the cardiovascular nuclei of the brain as well as in the intermediolateral cell column of spinal cord. Anatomical, neurophysiological, functional and pharmacological studies suggest that TRH is a neurotransmitter/neuromodulator in the central nervous system. Administration of TRH to experimental animals or human subjects induc...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2006
ISSN: 0021-9258
DOI: 10.1074/jbc.m600440200