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Subtype selectivity of a new α1-adrenoceptor antagonist, JTH-601: comparison with prazosin

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Abstract

The existence of α1-adrenoceptors with low affinity for prazosin (α1L group: α1L and α1N subtypes) has been proposed in addition to α1-adrenoceptor subtypes with high affinity for prazosin (α1H group: α1A, α1B and α1D subtypes). A newly synthesized α1-adrenoceptor antagonist, JTH-601 (N-(3-hydroxy-6-methoxy-2,4,5-trimethylbenzyl)-N-methyl-2-(4-hydroxy-2-isopropyl-5-methyl-phenoxy) ethylamine hemifumarate) showed approximately a 10 times higher affinity for the α1L group, a similar affinity for the α1A subtype, but a more than 10 times lower affinity for the α1B and α1D subtypes when compared with prazosin. These results provide a further pharmacological evidence that α1-adrenoceptors with low affinity for prazosin exist in addition to those with high affinity for prazosin, suggesting that JTH-601 may be useful for characterising the α1-adrenoceptor subtypes.

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