Pharmacological Profile of the 2-Alkynyladenosine Derivative 2-Octynylandenosine (YT-146) in the Cardiovascular System.

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We investigated the cardiovascular effects of 2-octynyladenosine (YT-146), an adenosine A<SUB>2</SUB> agonist, in various mammalian preparations in comparison with adenosine and 2-chloroadenosine. YT-146, when intravenously administered, caused a dose-dependent decrease of blood pressure in anesthetized normotensive rats (with ED<SUB>30</SUB> values of 0.4 μg/kg), and YT-146 was 250 times more potent than adenosine. Whereas adenosine and 2-chloroadenosine decreased heart rate at approximately equihypotensive doses, YT-146 had no negative chronotropic effects at hypotensive doses. Orally given YT-146 (0.1-1 mg/kg) produced a potent and long-lasting anti-hypertensive effect in spontaneously hypertensive rats. YT-146 was 15.9 and 12.5 times more potent than adenosine in producing relaxation of isolated porcine coronary arteries and in increasing dog coronary blood flow, respectively. Although YT-146 was equipotent to adenosine in causing a negative inotropic effect in isolated guinea pig atria, it was less potent than adenosine in producing atrioventricular conduction block in guinea pigs. On the other hand, 2-chloroadenosine was 9.1, 1.8 and 2.4 times more potent than adenosine in lowering blood pressure, relaxing isolated porcine coronary arteries and increasing dog coronary blood flow, respectively. 2-Chloroadenosine was the most potent in producing cardiodepression, i.e., negative inotropy and atrioventricular conduction block in guinea pigs. From these results, we concluded that YT-146 is a potent coronary vasodilator and also a potent, orally active and long-acting hypotensive agent having less cardiac depressant activity.
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Pharmacological Profile of the 2-Alkynyladenosine Derivative 2-Octynylandenosine (YT-146) in the Cardiovascular System.

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