1. The effects of veriloid and veratridine on right and left atrial receptors have been studied in cats. 2. Threshold doses of these drugs for right atrial receptors were found to be almost twice those for left atrial receptors. Beyond threshold doses, however, the dose-response curves were similar. 3. The sensitivity of left atrial receptors to veratridine was not altered by an increase in PCO2 and/or decrease in PO2 of left atrial blood. Therefore, the difference in the behaviour of left and right atrial receptors to these drugs is not due to the differences in PO2 and PCO2 of blood in the two atria. They are more likely to be a feature of the regenerative regions of the receptors.

01 Apr 1979·NeuropharmacologyQ2 · MEDICINE

Central antiemetic actions of pimozide and haloperidol in the dog

Q2 · MEDICINE

Article

Author: C.Y. Chai ; S.C. Wang ; P.M. Chung ; H.K. Lee

The 50% protective doses (PD₅₀) of oral and intracerebroventricular pimozide (I) [2062-78-4] against emesis or vomiting induced in conscious dogs by a threshold dose of i.v. apomorphine-HCl (0.01 mg/kg) were 5 μg/kg and 0.3 ng/kg resp., and the corresponding PD₅₀ values for haloperidol (II) [52-86-8] were 10 μg/kg orally and 0.3 ng/kg via the 4th ventricle.Oral I or II (100 μg/kg) prevented emesis induced by a threshold dose of apomorphine for an average of 6.6 and 4.2 days, resp.I or II (1 mg/kg, orally) completely inhibited emesis induced by levodopa or Hydergine (20 and 0.03 mg/kg i.v. resp.), and afforded moderate protection against emesis induced by CuSO₄ (40 mg orally); they had no effect on emesis induced by Veriloid or pilocarpine nitrate (0.01 and 1.0 mg/kg i.v. resp.).Thus, the primary site of antiemetic action of I and II is on the chemoreceptive emetic trigger zone in the area postrema of the medulla oblongata; however, at higher doses, depression of the vomiting center in the reticular formation of the medulla may also contribute.Oral I only afforded moderate protection against vomiting induced by morphine-HCl (1.0 or 2.0 mg/kg i.m.) and II was ineffective.Both I and II were ineffective against emesis induced by ouabain nitrate or acetylstrophanthidin, which act through the trigger zone, implying that either affinity of these agents at the receptor site is different or they act at different receptor sites within the trigger zone.

01 Dec 1978·European Journal of PharmacologyQ3 · MEDICINE

Mechanism of antiemetic action of penfluridol in the dog

Q3 · MEDICINE

Article

Author: Pao M. Chung ; Shih C. Wang ; Hsheng K. Lee

In conscious mongrel dogs, the 50% protective dose (PD₅₀) of intracerebroventricular (i.c.v., 4th ventricle) and oral (p.o.) penfluridol (I) [26864-56-2] against emesis induced by apomorphine (0.01 mg/kg i.v.) was 0.7 ng/kg and 1.5 μg/kg, resp., with a ratio of about 1 to 2000.Another striking feature of I as an antiemetic was its long duration of action.With a moderate oral dose, e.g. 10 μg/kg, the protective effect could last several days.I (1 mg/kg, orally), was extremely effective in raising the i.v. threshold emetic dose of apomorphine (1 mg/kg), levodopa (20 mg/kg), or Hydergine (0.09 mg/kg).With such a dose of I, however, the emetic threshold of oral CuSO₄ was not raised.Furthermore, I had no effect in preventing vomiting induced by Veriloid, peruvoside and pilocarpine.Apparently, the primary site of the antiemetic property of I is a selective action on the chemoceptive emetic trigger zone of the medulla.I afforded only moderate protection against vomiting induced by epinephrine, emetine, or Na salicylate, and was not effective against that induced by ouabain, acetylstrophanthidin, morphine, and nicotine.Since these emetic agents act principally through the trigger zone, this may imply that I administration is not equivalent to surgical ablation of this area.In addition, I only raised the threshold of emesis induced by apomorphine, levodopa and Hydergine, known to stimulate specifically the dopamine receptors.Furthermore, levodopa at a nonemetic i.v. dose was markedly effective in antagonizing the antiapomorphine action of I.Thus, I exerts its antiemetic action through an antidopaminergic activity.

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