Design-driven LO: the discovery of new ultra long acting dibasic beta2-adrenoceptor agonists.

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Connolly S, Alcaraz L, Bailey A, Cadogan E, Christie J, Cook AR, Fisher AJ, Hill S, Humphries A, Ingall AH, Kane Z, Paine S, Pairaudeau G, Stocks MJ, Young A

Design-driven LO: the discovery of new ultra long acting dibasic beta2-adrenoceptor agonists.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4612-6. doi: 10.1016/j.bmcl.2011.05.097. Epub 2011 Jun 13.

PubMed ID

21723724 [ View in PubMed

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Abstract

Starting with the molecular scaffold of the DA(2)/beta(2) dual agonist sibenadet (Viozan), a number of molecular changes were incorporated, which were designed to increase the potency and selectivity of the target molecule, and improve its pharmacokinetics. Through this process a novel, high potency, full beta(2)-agonist with high selectivity and long duration capable of being dosed once daily has been discovered.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Salmeterol	Beta-1 adrenergic receptor	EC 50 (nM)	794.33	N/A	N/A	Details
Salmeterol	Beta-1 adrenergic receptor	IC 50 (nM)	501.19	N/A	N/A	Details