Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.

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Barlocco D, Cignarella G, Piaz VD, Giovannoni MP, De Benedetti PG, Fanelli F, Montesano F, Poggesi E, Leonardi A

Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.

J Med Chem. 2001 Jul 19;44(15):2403-10.

PubMed ID

11448222 [View in PubMed

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Abstract

QSAR models have been used for designing a series of compounds characterized by a N-phenylpiperazinylalkylamino moiety linked to substituted pyridazinones, which have been synthesized. Measurements of the binding affinities of the new compounds toward the alpha(1a)-, alpha(1b)-, and alpha(1d)-AR cloned subtypes as well as the 5-HT(1A) receptor have been done validating, at least in part, the estimations of the theoretical models. This study provides insight into the structure activity relationships of the alpha(1)-ARs ligands and their alpha(1)-AR/5-HT(1A) selectivity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prazosin	Alpha-1A adrenergic receptor	Ki (nM)	0.61	N/A	N/A	Details
Prazosin	Alpha-1B adrenergic receptor	Ki (nM)	0.42	N/A	N/A	Details
Prazosin	Alpha-1D adrenergic receptor	Ki (nM)	0.23	N/A	N/A	Details