2336. Cizolirtine

Nomenclature

CAS number: 142155-43-9
N,N-Dimethyl-2-[(1-methyl-1H-pyrazol-5-yl)phenylmethoxy]ethanamine; 1-methyl-α-phenyl-O-(2-dimethylaminoethyl)-1H-pyrazole-5-methanol; E-3710.
C15H21N3O; mol wt 259.35.
C 69.47%, H 8.16%, N 16.20%, O 6.17%.

Description and references

Antinociceptive agent that inhibits release of calcitonin gene related peptide and substance P, q.v., from the spinal cord. Prepn: A. Colombo et al., EP 289380; eidem, US 5017596 (1988, 1991 both to Esteve). Prepn of isomers: J. A. Hueso-Rodriguez et al., Bioorg. Med. Chem. Lett. 3, 269 (1993). CE determn of chemical and enantiomeric purity: A. Gómez-Gomar et al., J. Chromatogr. A 950, 257 (2002). Pharmacology: I. Alvarez et al., Methods Find. Exp. Clin. Pharmacol. 22, 211 (2000). Mechanism of action study: S. Ballet et al., Neuropharmacology 40, 578 (2001). Clinical evaluation in chronic neuropathic pain: P. Shembalkar et al., Curr. Med. Res. Opin. 17, 262 (2001); in renal colic: I. Pavlik et al., Curr. Ther. 26, 1061 (2004). Review: N. Monck, Curr. Opin. Investig. Drugs 2, 1269-1272 (2001).

Chemical structure

Derivative

Citrate.

Nomenclature

CAS number: 142155-44-0
E-4018.
C15H21N3O.C6H8O7; mol wt 451.47.
C 55.87%, H 6.47%, N 9.31%, O 28.35%.

Therapeutic Category

Analgesic.

Keywords

Analgesic; Non-opioids