ARC 239 dihydrochloride hydrate is a selective α2B-AR adrenoceptor antagonist with a pKD value of 8.8. This antagonist is known to display inhibitory effects on α2A-AR (α2A) and α2D receptors with pKD values of 6.7 and 6.4 respectively. Studies indicate that ARC 239 dihydrochloride is 100-fold more selective towards the α2B-AR (α2B adrenoceptor) than chlorpromazine (sc-357313) and 7-hydroxychlorpromazine. Studies conducted on pentobarbital-treated dogs and rats show that ARC 239 dihydrochloride competitively antagonizes pressor responses to adrenaline, while inhibiting these pressor responses to noradrenaline, phenylephrine, tyramine, and dimethylphenylpiperazinium. ARC 239 dihydrochloride hydrate is an inhibitor of α2B-AR.
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