1. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation GPCR/G Protein
  2. nAChR Histamine Receptor
  3. Mecamylamine

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Mecamylamine hydrochloride) usually boasts enhanced water solubility and stability.

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Mecamylamine Chemical Structure

Mecamylamine Chemical Structure

CAS No. : 60-40-2

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Description

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].

IC50 & Target

nAChR[1], histamine receptor[2]

In Vitro

Mecamylamine (0.5-9 μM, bath administered) increases the firing frequency of identified 5-HT DRN (dorsal raphe nucleus) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: SCG neurons
Concentration: 10 μM
Incubation Time: 48 h
Result: Reduced the nicotine-facilitated increase in ERK1/2.
In Vivo

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 both β2 and α7 subunits[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 mice and α7 knockout mice, but decreased immobility time in wildtype littermates in the FST.
Clinical Trial
Molecular Weight

167.29

Formula

C11H21N

CAS No.
SMILES

CC1(C)C(NC)(C)C2CCC1C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mecamylamine
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