Does crude venom of the stonefish (Synanceia verrucosa) activate beta-adrenoceptors in the frog heart muscle?
Venom isolated from the stonefish Synanceia verrucosa was assayed in concentrations of 0.07 and 5.7 micrograms/ml on frog atrial fibres and myocytes. Venom, less than 2.9 micrograms/ml, dose-dependently increased the amplitude and the duration of the stimulated peak tension, lengthened the time constant of the relaxation phase and shortened the duration of the action potential (AP). The concentration of venom 5.7 micrograms/ml decreased the amplitude of the peak tension, induced a contracture, reduced the amplitude of the plateau and shortened its duration as well as the repolarizing phase of the AP. The positive inotropic effect induced by the venom (2.9 micrograms/ml) on the contraction was inhibited dose-dependently by propranolol but was unchanged by the alpha-adrenergic antagonists urapidil and yohimbine, the adenyl cyclase activity remaining sensitive to forskolin. Venom, adrenalin and propranolol competed for a common site. Venom (2.9 micrograms/ml) increased both the Ca and the delayed outward K currents of enzymatically isolated atrial myocytes. The data suggest that the venom activates adrenoceptors, essentially beta-adrenoceptors.
Sauviat
M P
MP
Unité INSERM 275, Ecole Polytechnique-ENSTA, Palaiseau, France.
Garnier
P
P
Goudey-Perriere
F
F
Perriere
C
C
D000200:Action Potentials / Q000187:drug effects; D000317:Adrenergic alpha-Antagonists / Q000378:metabolism / Q000494:pharmacology; D000319:Adrenergic beta-Antagonists / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D004305:Dose-Response Relationship, Drug; D005397:Fish Venoms / Q000008:administration & dosage / Q000378:metabolism / Q000633:toxicity*; D005399:Fishes; D006321:Heart / Q000187:drug effects*; D006325:Heart Atria / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D009206:Myocardium / Q000166:cytology; D010879:Piperazines / Q000494:pharmacology; D011433:Propranolol / Q000378:metabolism / Q000494:pharmacology; D011893:Rana esculenta; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D015016:Yohimbine / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D005397:Fish Venoms; D010879:Piperazines; D011943:Receptors, Adrenergic, beta; D015016:Yohimbine; D011433:Propranolol; C015568:urapidil