Hexamethonium bromide

Hexamethonium is a non-depolarising ganglionic blocker, a nicotinic nACh (NN) receptor antagonist.Target: nAChRHexamethonium is a non-depolarising ganglionic blocker, a nicotinic nACh receptor antagonist that acts in autonomic ganglia by binding mostly in or on the NN receptor, and not the acetylcholine binding site itself. It does not have any effect on the muscarinic acetylcholine receptors (mAChR) located on target organs of the parasympathetic nervous system but acts as antagonist at the nicotinic acetylcholine receptors located in sympathetic and parasympathetic ganglia (NN). Hexamethonium bromide is a nicotinic acetyl choline receptor antagonist. Induces apoptosis and inhibits the stimulatory effect of nicotine on endothelial cell DNA synthesis and proliferation. Hexamethonium bromide hydrate is an inhibitor of AChR α3 [1-3].

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[1]. Maneckjee, R. and J.D. Minna, Opioids induce while nicotine suppresses apoptosis in human lung cancer cells. Cell Growth Differ, 1994. 5(10): p. 1033-40.

[2]. Sanchez-Fortun, S., F. Sanz, and M.V. Barahona, Acute toxicity of several organophosphorous insecticides and protection by cholinergic antagonists and 2-PAM on Artemia salina larvae. Arch Environ Contam Toxicol, 1996. 31(3): p. 391-8.

[3]. Villablanca, A.C., Nicotine stimulates DNA synthesis and proliferation in vascular endothelial cells in vitro. J Appl Physiol (1985), 1998. 84(6): p. 2089-98.

PNU 282987 | Carbachol | GTS-21 | Methyllycaconitine citrate | Monepantel | PNU-120596 | Centrophenoxine hydrochloride | ZSET1446 | Aniracetam | Desformylflustrabromine hydrochloride | EVP-6124 (hydrochloride) | α-Lobeline Hydrochcloride | ABT 594 hydrochloride | Varenicline | Catharanthine

MOLECULAR FORMULA :

C12-H30-N2.2Br

MOLECULAR WEIGHT :

362.26

WISWESSER LINE NOTATION :

1K1&1&6K1&1&1 &E 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

2891 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

SKNEA7 Shionogi Kenkyusho Nenpo. Annual Report of Shionogi Research Laboratory. (Shionogi Seiyaku K.K. Kenkyusho, 5-12-4 Sagisu, Fukushima-ku, Osaka 553, Japan) No.1- 1951- Volume(issue)/page/year: 10,15,1960

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

200 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 78,708,1951

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

64130 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

SKNEA7 Shionogi Kenkyusho Nenpo. Annual Report of Shionogi Research Laboratory. (Shionogi Seiyaku K.K. Kenkyusho, 5-12-4 Sagisu, Fukushima-ku, Osaka 553, Japan) No.1- 1951- Volume(issue)/page/year: 10,15,1960

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

838 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,356,1982

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

70 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 91,1307,1971

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

78 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 91,1307,1971

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

22 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 2,233,1959

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rabbit

DOSE/DURATION :

50300 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

SKNEA7 Shionogi Kenkyusho Nenpo. Annual Report of Shionogi Research Laboratory. (Shionogi Seiyaku K.K. Kenkyusho, 5-12-4 Sagisu, Fukushima-ku, Osaka 553, Japan) No.1- 1951- Volume(issue)/page/year: 10,15,1960 ** REPRODUCTIVE DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

DOSE :

46 mg/kg

SEX/DURATION :

female 31-34 week(s) after conception

TOXIC EFFECTS :

Reproductive - Specific Developmental Abnormalities - gastrointestinal system Reproductive - Effects on Newborn - other neonatal measures or effects

REFERENCE :

ADCHAK Archives of Disease in Childhood. (British Medical Journal, POB 560B, Kennebunkport, ME 04046) V.1- 1926- Volume(issue)/page/year: 29,354,1954