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001-es BibID:BIBFORM047219
035-os BibID:(scopus)84878289088
Első szerző:Prokai-Tatrai Katalin
Cím:Design and Exploratory Neuropharmacological Evaluation of Novel Thyrotropin-Releasing Hormone Analogs and Their Brain-Targeting Bioprecursor Prodrugs / Katalin Prokai-Tatrai, Vien Nguyen, Szabolcs Szarka, Krisztina Konya, Laszlo Prokai
Dátum:2013
ISSN:1999-4923
Megjegyzések:Efforts to take advantage of the beneficial activities of thyrotropin-releasing hormone (TRH) in the brain are hampered by its poor metabolic stability and lack of adequate central nervous system bioavailability. We report here novel and metabolically stable analogs that we derived from TRH by replacing its amino-terminal pyroglutamyl (pGlu) residue with pyridinium-containing moieties. Exploratory studies have shown that the resultant compounds were successfully delivered into the mouse brain after systemic administration via their bioprecursor prodrugs, where they manifested neuropharmacological responses characteristic of the endogenous parent peptide. On the other hand, the loss of potency compared to TRH in a model testing antidepressant-like effect with a simultaneous preservation of analeptic activity has been observed, when pGlu was replaced with trigonelloyl residue. This finding may indicate an opportunity for designing TRH analogs with potential selectivity towards cholinergic effects.
Tárgyszavak:Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
bioprecursor prodrug
brain-targeting delivery
thyrotropin-releasing hormone
synthetic peptide analog
analeptic effect
antidepressant-like activity
Megjelenés:Pharmaceutics. - 5 : 2 (2013), p. 318-328. -
További szerzők:Nguyen, Vien Szarka Szabolcs Kónya Krisztina (1977-) (vegyész, kémia tanár) Prokai László
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