Prodrugs of Thyrotropin-Releasing Hormone and Related Peptides as Central Nervous System Agents
نویسندگان
چکیده
منابع مشابه
Prodrugs of thyrotropin-releasing hormone and related peptides as central nervous system agents.
Prodrug design for brain delivery of small- and medium-sized neuropeptides was reviewed, focusing on thyrotropin-releasing hormone and structurally related peptides as examples. We have summarized our most important advances in methodology, as well as assessed the benefits and limitations of bioreversible chemical manipulation techniques to achieve targeting of the parent molecules into the cen...
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The blood flow of thyroid, adrenal cortex and renal cortex in the pentobarbital anesthetized rat was assessed from hydrogen gas desaturation curve. The microcirculation of thyroid was markedly augmented within 2 min after an intraventricular injection of Thyrotropin-Releasing Hormone (TRH) while Met-Enkephalin (ENK) failed to influence. Both TRH and ENK stimulated the microcirculation of adrena...
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We employed quantitative autoradiography to examine the distribution of thyrotropin-releasing hormone (TRH) receptors in the rat CNS. The binding of [3H]3-methyl-histidine-TRH [( 3H]MeTRH) to TRH receptors in frozen rat brain sections was saturable, of a high affinity (Kd = 5 nM), and specific for TRH analogs. Autoradiograms of [3H]MeTRH binding showed highest concentrations of TRH receptors in...
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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...
متن کاملAssessment of thyrotropin-releasing hormone and thyrotropin reserve in man.
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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ژورنال
عنوان ژورنال: Molecules
سال: 2009
ISSN: 1420-3049
DOI: 10.3390/molecules14020633