methyl(2,3,3-trimethyltrinorbornan-2-yl)amine

Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area[1][2][5].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

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

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

nAChR[1], histamine receptor[2]

Mecamylamine (0.5-9 μM, bath administered) increases the firing frequency of identified 5-HT DRN neurons[1]. Mecamylamine (0.5-9 μM, bath administered) increases the glutamatergic and decreases the GABAergic input of 5-HT DRN neurons[1]. Mecamylamine (1 mM, 5 min) blocks the histamine receptor and the histamine-induced contractions in helically cut strips of rabbit aorta[2]. Mecamylamine (10 μM,48 h) attenuates the effect of nicotine’s action of neuroprotection[3]. Mecamylamine (1-100 nM, 30 min) dose-dependently attenuates endothelial tube formation in HDMVECs[4]. Western Blot Analysis[3] Cell Line: [3] Concentration: 10 μM Incubation Time: 48 h Result: Reduced the nicotine-facilitated increase in ERK1/2.

Mecamylamine (subcutaneous pumps, 50 mg/kg/day, 2 days) inhibits Choroidal neovascularization (CNV) in CNV mice model[4]. Mecamylamine (intraperitoneal injection, 0.5-1 mg/kg) has antidepressant-like effects in both the TST (tail suspension test) and FST (forced swim test) in C57BL/6J mice, which are dependent on bothβ2 andα7 subunits[5]. Animal Model: Choroidal neovascularization (CNV) mice model[1] Dosage: 50 mg/kg/day, 2 days Administration: Subcutaneous pumps implanted beneath the skin of the back), 200 μL and mean pumping rate of 0.5 μL/h. Result: Suppressed the development of CNV at Bruch’s membrane rupture sites in the absence of nicotine. Animal Model: C57BL/6J mice[5] Dosage: 0.5-1 mg/kg Administration: Intraperitoneal injection Result: Had no effect in β2 knockout miceand α7 knockout mice, but decreased immobility time in wildtype littermates in the FST.

[1]. Omar Hernández-González, et al. Mechanisms of stimulatory effects of mecamylamine on the dorsal raphe neurons. Brain Res Bull. 2020 Nov;164:289-298.

[2]. C P Robinson, et al. The influence of mecamylamine on contractions induced by different agonists and on the role of calcium ions in the isolated rabbit aorta. J Pharmacol Exp Ther. 1976 Apr;197(1):57-65.

[3]. Mahadevappa P Badanavalu, et al. Nicotine is neuroprotective to neonatal neurons of sympathetic ganglion in rat. Auton Neurosci. 2019 Jan;216:25-32.

[4]. Katsuji Kiuchi, et al. Mecamylamine suppresses Basal and nicotine-stimulated choroidal neovascularization. Invest Ophthalmol Vis Sci. 2008 Apr;49(4):1705-11.

[5]. Rabenstein RL, et al. The nicotinic antagonist mecamylamine has antidepressant-like effects in wild-type but not beta2- or alpha7-nicotinic acetylcholine receptor subunit knockout mice. Psychopharmacology (Berl). 2006 Dec;189(3):395-401.

MOLECULAR FORMULA :

C11-H21-N

MOLECULAR WEIGHT :

167.33

WISWESSER LINE NOTATION :

L55 ATJ CM1 C1 D1 D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

90 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

BCFAAI Bollettino Chimico Farmaceutico. (Societa Editoriale Farmaceutica, Via Ausonio 12, 20123 Milan, Italy) V.33- 1894- Volume(issue)/page/year: 103,490,1964

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

40 mg/kg

TOXIC EFFECTS :

Behavioral - sleep

REFERENCE :

AITEAT Archivum Immunologiae et Therapiae Experimentalis. (Ars Polona, POB 1001, 00-068 Warsaw 1, Poland) V.10- 1962- Volume(issue)/page/year: 10,905,1962

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

37500 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 25,163,1962

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

11900 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4168308