Inhalation by design: dual pharmacology beta-2 agonists/M3 antagonists for the treatment of COPD.

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Jones LH, Baldock H, Bunnage ME, Burrows J, Clarke N, Coghlan M, Entwistle D, Fairman D, Feeder N, Fulton C, Hilton L, James K, Jones RM, Kenyon AS, Marshall S, Newman SD, Osborne R, Patel S, Selby MD, Stuart EF, Trevethick MA, Wright KN, Price DA

Inhalation by design: dual pharmacology beta-2 agonists/M3 antagonists for the treatment of COPD.

Bioorg Med Chem Lett. 2011 May 1;21(9):2759-63. doi: 10.1016/j.bmcl.2010.10.132. Epub 2010 Oct 31.

PubMed ID

21075627 [ View in PubMed

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Abstract

This paper describes the successful design and development of dual pharmacology beta-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder using the principles of 'inhalation by design'. A key feature of this work is the combination of balanced potency and pharmacodynamic duration with desirable pharmacokinetic and material properties, whilst keeping synthetic complexity to a minimum.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tolterodine	Muscarinic acetylcholine receptor M3	Ki (nM)	3.6	N/A	N/A	Details