Corpus ID: 30160846

The pharmacological classification of practolol and chloropractolol.

  title={The pharmacological classification of practolol and chloropractolol.},
  author={Terry Kenakin and James W. Black},
  journal={Molecular pharmacology},
  volume={14 4},
The classification of beta adrenoceptor subtypes has apparently received substantial confirmation from the cardioselective properties of practolol, so-called beta 1 receptor blockade. This interpretation assumes that practolol has no relevant pharmacological properties other than beta receptor antagonism; the present report challenges that assumption. Practolol was studied to elucidate the reported alkylating properties of chloropractolol; although no evidence of alkylation was found, the… Expand
The Pharmacologic Estimation of Potencies of Agonists and Antagonists in the Classification of Adenosine Receptors
This chapter outlines some of the methods used to quantitate drug effects in isolated tissues for the purposes of adenosine receptor classification. There are advantages and disadvantages to studyingExpand
Comparative assessment ofβ-adrenoceptor blocking agents as simple competitive antagonists in isolated heart muscle: Similarity of inotropic and chronotropic blocking potencies against isoproterenol
Estimates of the equilibrium dissociation constants (KB) derived from the antagonism of the chronotropic and inotropic effects of isoproterenol were determined for fifteen β-adrenoceptor blocking agents of widely differing potency, and in no case was there a substantial difference between the inotropic and chronotropic values. Expand
Pharmacological Assay of Cardiac H2-Receptor Blockade by Amitriptyline and Lysergic Acid Diethylamide
Investigation of histamine responses of tachycardia in guinea pig right atrium and increased isometric tension in papillary muscle concludes that BOL, D-LSD, and amitriptyline are competitive antagonists of H-2-receptors in pharmacological assays, but other actions of these drugs distort or mask their measurement of H1-receptor affinity. Expand
The influence of molecular structure on the affinity and efficacy of some β-adrenoceptor agonists
Analysis of the structure-affinity and structure-efficacy relationships indicated that removal of the 3-hydroxyl group from the catechol ring reduces both affinity and efficacy without altering the selectivity of the drug for either β-adrenoceptor subtype. Expand
Persistent beta-adrenoceptor blockade with alkylating pindolol (BIM) in guinea-pig left atria and trachea.
The actions of alkylating pindolol (N8-bromoacetyl-N1-3'-(4-indolyloxy)-2'-hydroxypropyl[z]-1,8- diamino-p-menthane; BIM) have been examined on beta-adrenoceptors in guinea-pig left atria and trachea and changes in the maximal density were determined. Expand
Analysis of agonist dissociation constants as assessed by functional antagonism in guinea pig left atria.
There are serious limitations in the current theory for using functional antagonism as a means of obtaining agonist dissociation constants in electrically driven guinea pig left atria. Expand
The action of adrenoceptor agonists and antagonists on the guinea pig and dog trachea.
It is, therefore, unlikely that alpha 1-adrenoceptors play a major role in the excitation of the dog trachea under resting conditions whereas the participation of alpha 2-receptors in the mechanisms of adrenergic relaxation could not be ruled out. Expand
The results indicate that the bronchoconstrictor effects of these drugs are unrelated to β‐adrenoceptor blockade in the airway smooth muscle. Expand
The relative contribution of affinity and efficacy to agonist activity: organ selectivity of noradrenaline and oxymetazoline with reference to the classification of drug receptors
  • T. Kenakin
  • Chemistry, Medicine
  • British journal of pharmacology
  • 1984
Oxymetazoline demonstrated a pronounced organ selectivity, when compared to noradrenaline, by being a potent full agonist in rat anococcygeus muscle and a partial agonists in rat vas deferens, and theoretical modelling and experimental results indicate that high affinity/low efficacy agonists are much more sensitive to receptor coupling. Expand
The affinity and efficacy of the selective β1‐adrenoceptor stimulant RO363 at β1‐ and β2‐adrenoceptor sites
1 (−)−Isoprenaline and the selective β1‐adrenoceptor agonist RO363 were tested for their inotropic effects in left atrial (β1) and relaxant effects in K+‐depolarized uterine (β2) preparations fromExpand