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Molecules 2009, 14(2), 633-654; doi:10.3390/molecules14020633

Prodrugs of Thyrotropin-Releasing Hormone and Related Peptides as Central Nervous System Agents

1
Department of Pharmacology & Neuroscience, University of North Texas Health Science Center, Fort Worth, TX, USA
2
Department of Molecular Biology & Immunology, University of North Texas Health Science Center, Fort Worth, TX, USA
*
Author to whom correspondence should be addressed.
Received: 1 January 2009 / Revised: 21 January 2009 / Accepted: 5 February 2009 / Published: 6 February 2009
(This article belongs to the Special Issue Prodrugs)
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Abstract

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 central nervous system. The value of prodrug-amenable analogues as potential drug-like central nervous systems agents was highlighted.
Keywords: Neuropeptide; CNS-delivery; TRH; Analogue; Prodrug; Prodrug-amenable analogue Neuropeptide; CNS-delivery; TRH; Analogue; Prodrug; Prodrug-amenable analogue
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Prokai-Tatrai, K.; Prokai, L. Prodrugs of Thyrotropin-Releasing Hormone and Related Peptides as Central Nervous System Agents. Molecules 2009, 14, 633-654.

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