Potent M3 muscarinic receptor antagonist that displays ~ 120-fold selectivity over M2 receptors (Ki values are 4.2, 19 and 490nM for human M3, M1 and M2 receptors respectively). Exhibits >250-fold bronchial selectivity, inhibits ACh-induced bronchoconstriction but not ACh-induced bradycardia (KB values are 3.3 and 170 nM for rat trachea M3 and rat right atria M2 receptors respectively). Synonyms: (alphaR)-alpha-Cyclopentyl-alpha-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]benzeneacetamide Fumarate, (alphaR)-alpha-Cyclopentyl-alpha-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl]benzeneacetamide (2E)-2-Butenedioate (1:1) (salt) (9CI) CAS Number: 257603-40-0 Free Base: 244277-89-2 Molecular Formula: C24H36N2O2 (C4H4O4) Molecular Weight: 500.63 Purity: 99% (HPLC) Appearance: White solid Solubility: DMSO to 100mM, ethanol to 50mM Method for Determining Identity: Proton NMR Spectroscopic and Mass Spectrometric analysis TLC Conditions: Rf=0.52 (Dichloromethane: Methanol: Ammonia soln [9:1:0.05]) Microanalysis: Calculated: %C: 67.18, %H: 8.05, %N: 5.60 Optical Rotation: [a] = -7.7 (Concentration=1, Solvent=Methanol) Storage and Stability: Powder is stable for 6 months after receipt at 4C.
Molekulargewicht:
500.63
CAS Nummer:
[257603-40-0]
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