References of 6b,7b-Epoxy-3b-hydroxy-8-methyl-1aH,5aH-tropanium bromide di-2-thienylglycolate
Title: Tiotropium Bromide
CAS Registry Number: 136310-93-5
CAS Name: (1a,2b,4b,5a,7b)-7-[(Hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide
Synonyms: 6b,7b-epoxy-3b-hydroxy-8-methyl-1a
H,5a
H-tropanium bromide, di-2-thienylglycolate
Manufacturers' Codes: Ba-679 BR; Ba-679
Trademarks: Spiriva (Boehringer, Ing.)
Molecular Formula: C19H22BrNO4S2
Molecular Weight: 472.42
Percent Composition: C 48.31%, H 4.69%, Br 16.91%, N 2.96%, O 13.55%, S 13.57%
Literature References: Muscarinic receptor antagonist. Prepn: R. Banholzer
et al., EP 418716;
eidem,
US 5610163 (1991, 1997 both to Boehringer Ingelheim). Pharmacology: T. Takahashi
et al., Am. J. Respir. Crit. Care Med. 150, 1640 (1994). Binding study: E.-B. Haddad
et al., Mol. Pharmacol. 45, 899 (1994). Comparative clinical trial with salmeterol,
q.v., in chronic obstructive pulmonary disease (COPD): J. F. Donohue
et al., Chest 122, 47 (2002).
Properties: mp 218-220°.
Melting point: mp 218-220°
Therap-Cat: Bronchodilator.
Keywords: Bronchodilator; Quaternary Ammonium Compounds; Antimuscarinic.