Formulation: A solid
Formal Name: N-[1,1′-biphenyl]-2-yl-carbamic acid, 1-[2-[[4-[[4-(aminocarbonyl)-1-piperidinyl]methyl]benzoyl]methylamino]ethyl]-4-piperidinyl ester
Purity: ≥98%
Formula Markup: C35H43N5O4
Formula Weight: 597,8
Shelf life (days): 1460
CAS Number: 864750-70-9
Notes: TD-4208 is an antagonist of muscarinic acetylcholine receptors (mAChRs; Kis = 0.42, 0.3, 0.18, and 0.55 nM for M1, M2, M3, and M4 receptors, respectively, in membranes from CHO-K1 cells expressing the human receptors).{64970} It is selective for these receptors over M5 muscarinic receptors (Ki = 6.31 nM in membranes from CHO-K1 cells expressing the human receptor). TD-4208 inhibits calcium mobilization induced by acetylcholine (AChE; Item No. 23829) in CHO-K1 cells expressing M2 and M3 muscarinic receptors. It decreases AChE-induced contractions in isolated rat trachea in a concentration-dependent manner. TD-4208 decreases AChE-induced bronchoconstriction and reduces salivation induced by pilocarpine, a surrogate test for noisy breathing, in rats (ID50s = 45 and 1,164 µg/ml, respectively).{64971} It also decreases AChE-induced bronchoconstriction in dogs when administered intranasally at doses of 10 and 30 µg/kg. Formulations containing TD-4208 have been used in the treatment of chronic obstructive pulmonary disease (COPD).
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