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Vol. 290, Issue 2, 687-693, August 1999
3-Adrenoceptor Agonists1
Laboratoire de Physiopathologie et Pharmacologie Cellulaires et
Moléculaires, Institut National de la Santé et de la
Recherche Médicale, Nantes Cedex, France (C.G., J.-N.T., V.L.,
K.L., D.E., H.L.M.); Institut National de la Santé et de la
Recherche Médicale U-317, Institut Louis Bugnard, Faculté
de Médecine, Université Paul Sabatier, Toulouse Cedex,
France (G.T., D.L.); and Faculté des Sciences et Techniques,
Université de Nantes, Nantes Cedex, France (C.G.)
The aim of the present study was to compare the effects of three
preferential (BRL 37344, SR 58611, CL 316 243) and a partial (CGP
12177) 
-adrenoceptor (3-AR) agonists on the
contractility of ventricular strips sampled from various mammalian
species including humans. In the human heart, all 3-AR
agonists tested decreased contractility by 40 to 60% below control
with an order of potency: BRL 37344 > CL 316 243 = SR 58611 
CGP 12177. In the dog, the negative inotropic effects produced by
3-AR stimulation were less pronounced than in humans,
30% below control. The order of potency of 3-AR
agonists was CGP 12177 > BRL 37344 = SR 58611 CL 316 243; i.e., very different from that observed in humans. In rat, only
BRL 37344 was efficient to decrease contractility. In guinea pig, only
CL 316 243 significantly reduced peak tension. In both species, the
reduction in peak tension did not exceed 20 to 30%. Finally, in the
ferret, none of the agonists tested induced a negative inotropic
effect. In dog, the negative inotropic effects of CGP 12177 were not
modified by nadolol, but were abolished by bupranolol, a
1-3-AR. 3-AR transcripts were detected in the dog but not in the rat ventricle by using a reverse
transcription-polymerase chain reaction assay. We conclude that cardiac
negative inotropic effects related to 3-AR
agonist stimulation vary markedly depending on the species. A
comparable interspecies variation previously has been reported
concerning the lipolytic effects of 3-AR agonist stimulation. Our study demonstrates that the pharmacological profile of
a 3-AR agonist on the human myocardium cannot be
extrapolated from usual animal models.
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