Design and synthesis of a fluorescent muscarinic antagonist.

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Jones LH, Randall A, Napier C, Trevethick M, Sreckovic S, Watson J

Design and synthesis of a fluorescent muscarinic antagonist.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.

PubMed ID

18042383 [ View in PubMed

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Abstract

The design and concise synthesis of a fluorescent tolterodine-BODIPY (boron dipyrromethene) conjugate is described which possesses potent antimuscarinic activity. This derivative illustrates proof-of-concept for the preparation of other useful fluorophoric antimuscarinic agents which have potential utility in receptor occupancy studies and high throughput screens.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tolterodine	Muscarinic acetylcholine receptor M1	Ki (nM)	1.4	N/A	N/A	Details
Tolterodine	Muscarinic acetylcholine receptor M2	Ki (nM)	2.7	N/A	N/A	Details
Tolterodine	Muscarinic acetylcholine receptor M3	Ki (nM)	3.6	N/A	N/A	Details
Tolterodine	Muscarinic acetylcholine receptor M4	Ki (nM)	3.1	N/A	N/A	Details
Tolterodine	Muscarinic acetylcholine receptor M5	Ki (nM)	2.2	N/A	N/A	Details