Inhibition of nicotine-induced relaxation of the bovine retractor penis muscle by compounds known to have ganglion-blocking properties.
1. The relative potency in blocking the nicotine-induced relaxation of the bovine retractor penis muscle (BRP) was estimated for 12 drugs known to have ganglion-blocking properties. 2. The order of potency of the drugs studied was mecamylamine greater than chlorisondamine greater than pentolinium greater than propantheline greater than (+)-tubocurarine greater than hexamethonium greater than emepronium greater than tetraethylammonium greater than glycopyrrolate greater than decamethonium greater than butylscopolamine greater than scopolamine. 3. The results conform well to those obtained with other pharmacological methods used for the estimation of ganglion-blocking activity. 4. It is concluded that blockade of the nicotinic relaxation of the BRP can be used as an alternative method for quantitative assessment of ganglion-blocking activity. 5. Advantages of this technique are that it discriminates well between antinicotinic and antimuscarinic activity and that it satisfies most or all ethical and economical demands. 6. It is also possible that this method has certain value in predicting whether a drug has enough ganglion-blocking activity to be likely to cause impotence.
Alaranta
S
S
Department of Pharmacy, University of Helsinki, Finland.
Klinge
E
E
Pätsi
T
T
Sjöstrand
N O
NO
D000818:Animals; D002417:Cattle; D005730:Ganglionic Blockers / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D009126:Muscle Relaxation / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009466:Neuromuscular Blocking Agents / Q000494:pharmacology; D009538:Nicotine / Q000037:antagonists & inhibitors*; D010413:Penis / Q000187:drug effects*; D011976:Receptors, Muscarinic / Q000187:drug effects; D012044:Regression Analysis
D005730:Ganglionic Blockers; D009466:Neuromuscular Blocking Agents; D011976:Receptors, Muscarinic; D009538:Nicotine