Inhibition via opioid ?-and ?-receptors of vagal transmission in rabbit isolated heart

Abstract
The nervi vagi of isolated perfused rabbit hearts were stimulated by 10 s trains of electrical pulses at 1,2 or 5 Hz. Morphine, Met-enkephalin and D-Ala2,D-Leu5-enkephalin reduced the ensuing bradycardia with IC50 values of 148, 25 and 3.2 nM, respectively. Naloxone antagonized the effects of morphine and Met-enkephalin; KB values (dissociation constants of antagonist-receptor complex) were 1.1 and 33 nM, respectively. The δ-receptorselective antagonist ICI 174864 antagonized Met-enkephalin, KB 28 nM, but at 0.2 μM did not antagonize morphine. It is concluded that vagal transmission to the rabbit heart can be inhibited by activation of both opioid μ-und δ-receptors.

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