Synthesis and evaluation of in vivo anti‐hypothermic effect of all stereoisomers of the thyrotropin‐releasing hormone mimetic: Rovatirelin Hydrate

2019 ◽  
Vol 25 (12) ◽  
Author(s):  
Naotake Kobayashi ◽  
Norihito Sato ◽  
Katsuji Sugita ◽  
Kouji Takahashi ◽  
Tamio Sugawara ◽  
...  
Keyword(s):  
Thyrotropin Releasing Hormone ◽  
Releasing Hormone ◽  
Hypothermic Effect

Systemic administration of thyrotropin-releasing hormone enhances striatal dopamine release in vivo

1990 ◽  
Vol 536 (1-2) ◽  
pp. 347-352 ◽  
Author(s):  
Michael R. Kreutz ◽  
Ian N. Acworth ◽  
Hendrik Lehnert ◽  
Richard J. Wurtman
Keyword(s):  
Dopamine Release ◽  
Systemic Administration ◽  
Thyrotropin Releasing Hormone ◽  
Striatal Dopamine ◽  
Releasing Hormone ◽  
Striatal Dopamine Release

scholarly journals Brain Delivery of Thyrotropin-Releasing Hormone via a Novel Prodrug Approach

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 349 ◽  
Author(s):  
Katalin Prokai-Tatrai ◽  
Daniel L. De La Cruz ◽  
Vien Nguyen ◽  
Benjamin P. Ross ◽  
Istvan Toth ◽  
...  
Keyword(s):  
Brain Homogenate ◽  
Thyrotropin Releasing Hormone ◽  
Metabolic Stability ◽  
Antidepressant Effect ◽  
Brain Delivery ◽  
Small Peptides ◽  
Releasing Hormone ◽  
Membrane Affinity

Using thyrotropin-releasing hormone (TRH) as a model, we explored whether synergistic combination of lipoamino acid(s) and a linker cleaved by prolyl oligopeptidase (POP) can be used as a promoiety for prodrug design for the preferential brain delivery of the peptide. A representative prodrug based on this design principle was synthesized, and its membrane affinity and in vitro metabolic stability, with or without the presence of a POP inhibitor, were studied. The in vivo formation of TRH from the prodrug construct was probed by utilizing the antidepressant effect of the peptide, as well as its ability to increase acetylcholine (ACh) synthesis and release. We found that the prototype prodrug showed excellent membrane affinity and greatly increased metabolic stability in mouse blood and brain homogenate compared to the parent peptide, yet a POP inhibitor completely prevented prodrug metabolism in brain homogenate. In vivo, administration of the prodrug triggered antidepressant-like effect, and microdialysis sampling showed greatly increased ACh release that was also antagonized upon a POP inhibitor treatment. Altogether, the obtained promising exploratory data warrant further investigations on the utility of the prodrug approach introduced here for brain-enhanced delivery of small peptides with neurotherapeutic potential.

In vivo Release of Dopamine, Luteinizing Hormone-Releasing Hormone and Thyrotropin-Releasing Hormone in Male Rats Bearing a Prolactin-Secreting Tumor

1987 ◽  
Vol 46 (2) ◽  
pp. 110-116 ◽  
Author(s):  
James L. Voogt ◽  
Wim J. de Greef ◽  
Theo J. Visser ◽  
Jurien de Koning ◽  
Jan T.M. Vreeburg ◽  
...  
Keyword(s):  
Luteinizing Hormone ◽  
Thyrotropin Releasing Hormone ◽  
Male Rats ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
In Vivo Release

Release of Thyrotropin and Prolactin by a Thyrotropin-Releasing Hormone (TRH) Precursor, TRH-Gly: Conversion to TRH Is Sufficient for in vivo Effects

1990 ◽  
Vol 52 (6) ◽  
pp. 618-625 ◽  
Author(s):  
Eugene Pekary ◽  
Robert Stephens ◽  
Marie Simard ◽  
Xuan-Ping Pang ◽  
Vierka Smith ◽  
...  
Keyword(s):  
Thyrotropin Releasing Hormone ◽  
Releasing Hormone ◽  
In Vivo Effects

A Study of the Effect of the Thyrotropin-Releasing Hormone Metabolite, Histidyl-Proline Diketopiperazine, on Prolactin Secretion in Vivo*

Endocrinology ◽  
1981 ◽  
Vol 109 (5) ◽  
pp. 1375-1379 ◽  
Author(s):  
CHARLES H. EMERSON ◽  
SHARON ALEX ◽  
LEWIS E. BRAVERMAN ◽  
MARJORIE S. SAFRAN
Keyword(s):  
Prolactin Secretion ◽  
Thyrotropin Releasing Hormone ◽  
Releasing Hormone
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