These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Pharmacology of ASL-8052, a novel beta-adrenergic receptor antagonist with an ultrashort duration of action.
    Author: Gorczynski RJ, Shaffer JE, Lee RJ.
    Journal: J Cardiovasc Pharmacol; 1983; 5(4):668-77. PubMed ID: 6193366.
    Abstract:
    ASL-8052, a novel beta-adrenergic receptor antagonist, was studied in isolated guinea pig cardiac and tracheal tissues, in isolated frog sciatic nerves, and in anesthetized dogs. The compound was a moderately potent beta-adrenoceptor antagonist in right atria (pA2 6.96) but was much less active in tracheal tissues (pA2 5.33), indicating cardioselective properties. ASL-8052 possessed a small degree of intrinsic sympathomimetic action in isolated guinea pig right atria and caused direct cardiac depression only at concentrations 1,000-fold higher than its cardiac pA2. Significant local anesthetic action in frog sciatic nerve occurred at extremely high concentrations of ASL-8052 (greater than 0.1 M). In anesthetized dogs, ASL-8052 produced steady-state levels of beta-blockade within 10 min during a 3-h intravenous infusion. In contrast, propranolol produced increasing levels of blockade throughout most of the infusion period. Recovery from beta-blockade occurred rapidly following termination of ASL-8052 infusion (80% recovery in approximately 12 min), whereas very little recovery occurred following cessation of propranolol infusion. Intravenous infusion of ASL-8052 produced dose-dependent blockade of cardiac responses to isoproterenol but only minimally decreased hindlimb vascular responses to isoproterenol. The results indicate that ASL-8052 is a novel cardioselective beta-blocker with an ultrashort duration of action.
    [Abstract] [Full Text] [Related] [New Search]