Pharmacological properties of a new antiasthmatic xanthine derivative devoid of central stimulatory activity.

Abstract	The bronchodilating effect and other related pharmacological properties of an 8-amino alkyl substituted xanthine (S 9795) were compared with those of reference drugs, in particular theophylline. The in vitro studies using the tracheal ring, taenia coli, rat peritoneal mastocytes and enzymic preparations demonstrated the potency of S 9795 as an antiasthmatic drug, possessing protective activity superior to that of theophylline and enprofylline. S 9797 was 100 times more active as a cAMP phosphodiesterase inhibitor than theophylline. The compound also protected against mast cell degranulation and consequent release of spasmogen due to antigen-antibody reaction or induced by Ca2+ movements. Given orally or intravenously. S 9795 had a highly selective protective effect against bronchoconstriction induced by pharmacological reagents or allergic reactions with no demonstrable effect on the central nervous or cardiovascular systems. The pharmacological effects of S 9795 were of longer duration than those of theophylline and enprofylline. These studies demonstrate the potential therapeutic value of S 9795 in the therapy of bronchospastic disorders.
Authors	J Duhault, M Boulanger, M Lonchampt, F Tisserand, S Holstorp, G Saint-Romas, L Pennel, G Regnier
Journal	Arzneimittel-Forschung (Arzneimittelforschung) Vol. 37 Issue 12 Pg. 1353-62 (Dec 1987) ISSN: 0004-4172 [Print] Germany
PMID	2835053 (Publication Type: Comparative Study, Journal Article)
Chemical References	Bronchodilator Agents Xanthines S 9795 Theophylline 3',5'-Cyclic-AMP Phosphodiesterases
Topics	3',5'-Cyclic-AMP Phosphodiesterases (antagonists & inhibitors) Animals Asthma (drug therapy) Behavior, Animal (drug effects) Blood Pressure (drug effects) Bronchodilator Agents (pharmacology) Colon (drug effects) Dogs Female Guinea Pigs Heart Rate (drug effects) Male Mast Cells (drug effects) Mice Muscle Contraction (drug effects) Rats Rats, Inbred Strains Respiration (drug effects) Theophylline (pharmacology, therapeutic use) Trachea (drug effects) Xanthines (pharmacology, therapeutic use)

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