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J Med Chem. 2010 Feb 25;53(4):1871-5. doi: 10.1021/jm9018349.

Engineering galanin analogues that discriminate between GalR1 and GalR2 receptor subtypes and exhibit anticonvulsant activity following systemic delivery.

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1
Department of Medicinal Chemistry, College of Pharmacy, University of Utah, 421 WakaraWay, Salt Lake City, Utah 84108, USA.

Abstract

Galanin modulates seizures in the brain through two galanin receptor subtypes, GalR1 and GalR2. To generate systemically active galanin receptor ligands that discriminate between GalR1 and GalR2, the GalR1-preferring analogue Gal-B2 (or NAX 5055) was rationally redesigned to yield GalR2-preferring analogues. Systematic truncations of the N-terminal backbone led to [N-Me,des-Sar]Gal-B2, containing N-methyltryptophan. This analogue exhibited 18-fold preference in binding toward GalR2, maintained agonist activity, and exhibited potent anticonvulsant activity in mice following intraperitoneal administration.

PMID:
20121116
PMCID:
PMC2846716
DOI:
10.1021/jm9018349
[Indexed for MEDLINE]
Free PMC Article
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