A NEW GUANIDINE DERIVATIVE: DISSOCIATION OF THE ADRENERGIC NEURON BLOCKING ACTIVITY FROM LOCAL ANESTHETIC ACTIVITY
| Autor: | Hiroaki Nishio, Teruko Hosotani, Sachiyuki Hamano, Yoshimi Misu |
|---|---|
| Rok vydání: | 1976 |
| Předmět: |
Male
Chronotropic medicine.drug_class Adrenergic Blood Pressure Stimulation Adrenergic Neurons Pharmacology Guanidines Norepinephrine Procaine Dogs medicine Animals Heart Atria Anesthetics Local Guanethidine Neurons Chemistry Local anesthetic Myocardium Parasympatholytics Rats Anesthetic Female Rabbits Spleen medicine.drug |
| Zdroj: | Japanese Journal of Pharmacology. 26:367-375 |
| ISSN: | 0021-5198 |
| Popis: | Effects of 4-7-exo-methylene-hexahydroisoindoline-ethyl-guanidine hemisulfate (No. 865-123), a new guanidine derivative, on adrenergic neurons and its local anesthetic activity were investigated in comparison with guanethidine. Both derivatives produced in a dose-dependent manner a progressive irreversible reduction of positive chronotropic and contractile responses to postganglionic sympathetic nerve stimulation in isolated rabbit atria. The time course of the reduction by No. 865-123 was somewhat slower. In dogs administered both agents, the pressor response to carotid occlusion was reduced and that to exogenous noradrenaline was potentiated with a slight decrease in blood pressure. Noradrenaline stores in the heart and spleen of rats were also depleted to a similar extent. In the guinea pig weal method, guanethidine acted as a potent local anesthetic with a slow onset and a prolonged action as compared to procaine. No. 865-123 revealed no more anesthetic activity than did saline. It is unlikely that the local anesthetic activity of the guanidine derivatives contributes to the adrenergic neuron blocking activity. |
| Databáze: | OpenAIRE |
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