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Trh analogs show enhanced central nervous system selectivity because of increased biological stability


, : Trh analogs show enhanced central nervous system selectivity because of increased biological stability. Regulatory Peptides 2(5): 277-284

TRH exerts both endocrinological and neuropharmacological actions. Two analogs of TRH, L-trans-3-methylprolinamide and L-3,3-dimethylprolinamide were examined for their neuropharmacological and endocrinological effects. Comparisons of their ability to provoke hyperthermia in rabbits demonstrated that both analogs were more potent than TRH, but like the parent peptide had only a limited ability to cross the blood brain barrier. This conclusion was confirmed by whole body autoradiographical studies. Both analogs had a similar potency to TRH with respect to the ability to provoke TSH release. The increased potency in neuropharmacological tests results from enhanced bioavailability to CNS sites. A similar rationale can be used to explain the CNS selectivity claimed in the literature for other analogs of TRH.

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