Nomenclature
CAS number: 15500-66-0
1,1′-[(2β,3α,5α,16β,17β)-3,17-Bis(acetyloxy)androstane-2,16-diyl]bis[1-methylpiperidinium]
dibromide; 1,1′-(3α,17β-dihydroxy-5α-androstan-2β,16β-ylene)bis[1-methylpiperidinium]
dibromide diacetate; 3α,17β-diacetoxy-2β,16β-dipiperidino-5α-androstane dimethobromide; 2β,16β-dipiperidino-5α-androstane-3α,17β-diol diacetate dimethobromide; poncuronium bromide (rescinded USAN); NA-97; Org-NA-97; Mioblock (Sankyo); Pavulon (Organon).
C
35H
60Br
2N
2O
4; mol wt 732.67.
C 57.38%, H 8.25%, Br 21.81%, N 3.82%, O 8.73%.
Description and references
Aminosteroid, competitive neuromuscular blocker.
Prepn: W. R. Buckett et al., Chim. Ther. 2, 186 (1967); eidem, J. Med. Chem. 16, 1116 (1973). Structural studies: Savage et al., J. Chem. Soc. B 1971, 410. Structure-activity
correlation: Waser, Anaesthesist 20, 23 (1971). Pharmacology: W. R. Buckett, I. L. Bonta, Fed. Proc. 25, 718 (1966); W.
R. Buckett et al., Br. J. Pharmacol.
Chemother. 32, 671 (1968); I. L. Bonta et al., Eur. J. Pharmacol. 4, 83, 303 (1968). Comparative study of neuromuscular
blocking and vagolytic effect: S. L. Son et al., Anesthesiology 55, 12 (1981).
Review: Speight, Avery, Drugs 4, 163-226 (1972).
Properties
Odorless crystals with bitter taste, mp 215°. One gram dissolves in 30
parts chloroform, one part water (20°). LD50 in mice (mg/kg): 0.047 i.v.; 0.152 i.p.; 0.167 s.c.; 21.9 orally; in rats, rabbits: 0.153, 0.016 i.v. (Buckett, 1968).Therapeutic Category
Neuromuscular blocking agent.
Therapeutic Category (Veterinary)
Neuromuscular blocking agent.
Keywords
Neuromuscular Blocking Agent; Nondepolarizing Agents