Enhancement of availability of cloricromene at brain level by a lipophilic prodrug-Reference-Cited by-同舟云学术

Enhancement of availability of cloricromene at brain level by a lipophilic prodrug

Published:2006-07 Issue:7 Volume:58 Page:1001-1005
ISSN:0022-3573
Container-title:Journal of Pharmacy and Pharmacology
language:en
Short-container-title:

Author:

Pignatello R¹,Maltese A²,Maugeri F²,Bucolo C²

Affiliation:

1. Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, Viale A. Doria, 6, 95125 Catania, Italy

2. Dipartimento di Farmacologia Sperimentale e Clinica, Università degli Studi di Catania, Viale A. Doria, 6, 95125 Catania, Italy

Abstract

Abstract The pharmacokinetics of a lipophilic alkylamino acid (LAA) prodrug of cloricromene (AD6), namely CLOR-C4, was studied in rat plasma and brain. In particular, we observed that the intraperitoneal administration of CLOR-C4 to rats was able to provide a slight but statistically significant higher concentration of the active drug metabolite (cloricromene acid) in the brain compared with the parent drug administered by the same way. The correlation between pharmacokinetic data and calculated partition (LogP) and brain distribution coefficients (LogBB) supported the hypothesis that the amphiphilic nature of the LAA promoiety could be responsible for a better penetration into the brain, more than the simple increase of lipophilicity gained with respect to the parent drug.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Link

http://academic.oup.com/jpp/article-pdf/58/7/1001/36736398/jpp.58.7.0017.pdf

Reference22 articles.

1. Synthesis, structure elucidation, in vitro biological activity, toxicity, and Caco-2 cell permeability of lipophilic analogues of alpha-conotoxin MII;Blanchfield;J. Med. Chem.,2003

2. Multiple actions of the coumarine derivative cloricromene and its protective effects on ischemic brain injury;Calapai;Naunyn. Schmiedebergs Arch. Pharmacol.,1995

3. Prediction of intestinal absorption and blood-brain barrier penetration by computational methods;Clark;Comb. Chem. High Throughput Screen.,2001

4. Cloricromene, a coumarine derivative, protects against collagen-induced arthritis in Lewis rats;Cuzzocrea;Br. J. Pharmacol.,2000

5. Functional implications of modifying RyR-activating peptides for membrane permeability;Dulhunty;Br. J. Pharmacol.,2005

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