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]. 2nd communication: investigations on theophylline-like activities
| Autor: | E G, Mikus, Z, Kapui, D, Korbonits, K, Boér, E, Boronkay, J, Gyürky, J, Révész, F, Lacheretz, M, Pascal, P, Arányi |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Male
Oxadiazoles Guinea Pigs Hemodynamics Histamine Antagonists Receptors Purinergic P1 In Vitro Techniques Autonomic Nervous System Bronchodilator Agents Rats Electrophysiology Antitussive Agents Theophylline Purines Respiratory Mechanics Animals Female Rats Wistar 2' 3'-Cyclic-Nucleotide Phosphodiesterases |
| Zdroj: | Arzneimittel-Forschung. 47(12) |
| ISSN: | 0004-4172 |
| Popis: | 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) is a new xanthine derivative, structurally related to theophylline. Potent antitussive activity in the 4 to 8 mg/kg dose range, by the oral route, was already demonstrated for this compound. In the present work, it is shown that contrary to theophylline, CH-13584 does not interact with adenosine A1 receptor and is a weaker inhibitor of cyclic nucleotide phosphodiesterase. In addition, CH-13584 is a less active bronchodilator in vitro and in vivo. It is also devoid of the cardiovascular and behaviour side-effects of theophylline and of effects on diuresis at dosage well above the antitussive dose. CH-13584, therefore, has a different pharmacological profile compared to theophylline and is devoid of the known side-effects of the latter. Such differences could result from a different biochemical profile. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|