NDLI: Inhibition of the development of morphine tolerance by a potent dual mu-delta-opioid antagonist, H-Dmt-Tic-Lys-NH-CH2-Ph.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Jinsmaa, Yunden Marczak, Ewa D. Balboni, Gianfranco Salvadori, Severo Lazarus, Lawrence H.
Description	Country affiliation: United States Author Affiliation: Jinsmaa Y ( Medicinal Chemistry Group, Laboratory of Pharmacology, National Institute of Environmental Health Sciences, Research Triangle Park, North Carolina 27709, USA.)
Abstract	Three analogues of the dual mu-/delta-antagonist, H-Dmt-Tic-R-NH-CH2-Ph (R = 1, Lys-Z; 2, Lys-Ac; 3, Lys) were examined in vivo: 1 and 2 exhibited weak bioactivity, while 3 injected intracerebroventricularly was a potent dual antagonist for morphine- and deltorphin C-induced antinociception comparable to naltrindole (delta-antagonist), but 93% as effective as naloxone (nonspecific opioid receptor antagonist) and 4% as active as CTOP, a mu antagonist. Subcutaneous or oral administration of 3 antagonized morphine-induced antinociception indicating passage across epithelial and blood-brain barriers. Mice pretreated with 3 before morphine did not develop morphine tolerance indicative of a potential clinical role to inhibit development of drug tolerance.
File Format	HTM / HTML
ISSN	00913057
e-ISSN	18735177
DOI	10.1016/j.pbb.2008.05.008
Journal	Pharmacology Biochemistry and Behavior
Issue Number	4
Volume Number	90
Language	English
Publisher	Elsevier
Publisher Date	2008-10-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Discipline Behavioral Sciences Discipline Biochemistry Discipline Pharmacology Analgesics, Opioid Pharmacology Morphine Oligopeptides Receptors, Opioid, Delta Antagonists & Inhibitors Receptors, Opioid, Mu Animals Area Under Curve Dose-response Relationship, Drug Drug Tolerance Injections, Intraventricular Injections, Subcutaneous Ligands Mice Naltrexone Analogs & Derivatives Narcotic Antagonists Reaction Time Drug Effects Somatostatin Research Support, N.i.h., Extramural Research Support, N.i.h., Intramural Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Biological Psychiatry Behavioral Neuroscience Biochemistry Clinical Biochemistry Toxicology Pharmacology

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