Disease relevance of ARC239

• AR-C239 did not change the tachycardia induced by stimulation of the cardiac nerve in dogs and, at least in this preparation, seems to be a specific alpha 1-adrenoceptor blocking drug [1].
• Effect of hypertension and age on alpha 1-adrenoceptors in rat brain: modulation of [3H] prazosin binding by chronic treatment with desipramine and AR-C239 [2].

High impact information on ARC239

• The first class of binding sites interacts preferentially with the postsynaptic alpha-adrenoceptor blocker ARC239, as can be expected for postsynaptic alpha-adrenoceptors [3].
• When administered into the cisterna magna of dogs, AR-C239 did not have any centrally mediated cardiovascular actions and heart rate [1].
• AR-C239 did not modify the functioning of the baroreflex arc [1].
• Injected intravenously into closed-chest dogs, AR-C239 (3-50 micrograms/kg) induced a progressive fall in blood pressure, heart rate, and sympathetic nerve activity [1].
• Repeated AR-C239 treatment did not alter [3H] prazosin binding in senescent Wistar-Kyoto and mature spontaneously hypertensive rats, but significantly increased the [3H] prazosin binding density in mature Wistar-Kyoto rats [2].

References