Cayman TD-4208

TD-4208 is an antagonist of muscarinic acetylcholine receptors (mAChRs; K_is = 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).¹ It is selective for these receptors over M₅ muscarinic receptors (K_i = 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).² 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).

WARNING This product is not for human or veterinary use.