Experimental studies on the antitussive properties of the new xanthine derivative 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl) methyl]. 3rd communication: examinations on opioid mechanisms and physical drug dependence.

Abstract	CH-13584 (formerly: KHL-8425, 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7[(5-methyl-1,2,4-oxadiazol-3-yl)methyl], CAS 115779-20-9) showed antitussive effect on the citric acid spray-induced cough model. The antitussive effect of p.o. CH-13584 was antagonised by i.m. or intracerebroventricular (i.c.v.) naloxone, i.m. nor-binaltorphimine or s.c. beta-funaltrexamine. Intracerebroventricular administration of CH-13584 induced long-lasting antitussive effect which was antagonised by coadministration of i.c.v. naloxone. CH-13584 did not bind to opioid mu, delta, kappa receptor in vitro or inhibit the [3H]diprenorphine binding in vivo. Two-week treatment with CH-13584 up to the dose of 100 mg/kg p.o. did not produce autonomic and behavioural signs of withdrawal induced either by drug withdrawal or by naloxone injection, while morphine and codeine induced characteristic opioid-type physical dependence in rats.
Authors	Z Kapui, E G Mikus, J Bence, K Gerber, K Boér, D Korbonits, A Borsodi, P Arányi
Journal	Arzneimittel-Forschung (Arzneimittelforschung) Vol. 48 Issue 12 Pg. 1147-55 (Dec 1998) ISSN: 0004-4172 [Print] Germany
PMID	9893929 (Publication Type: Journal Article)
Chemical References	Antitussive Agents Narcotic Antagonists Oxadiazoles Purines Receptors, Opioid 1H-purine-2,6-dione, 3,7-dihydro-3-methyl-7-((5-methyl-1,2,4-oxadiazol-3-yl)methyl)-
Topics	Animals Antitussive Agents (adverse effects, pharmacokinetics, pharmacology) Binding, Competitive (drug effects) Cough (chemically induced, prevention & control) Guinea Pigs Injections, Intraventricular Male Mice Narcotic Antagonists (pharmacology) Oxadiazoles (adverse effects, pharmacokinetics, pharmacology) Purines (adverse effects, pharmacokinetics, pharmacology) Rats Rats, Wistar Receptors, Opioid (drug effects) Substance Withdrawal Syndrome Substance-Related Disorders (physiopathology)

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