Mecamylamine
Based on 7 publication(s) in Google Scholar
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.
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- No. CAS: 60-40-2
- Fòrmula: C11H21N
- Peso molecular:167.29
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | IC50 |
1.8 μM
Compound: 5, mecamylamine
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Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
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[PMID: 9435889] |
| PC-12 | EC50 |
0.2 μM
Compound: 5, mecamylamine
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Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
Compound was evaluated for functional potency and efficacy at rat Nicotinic acetylcholine receptor in PC12 cells (ganglionic)
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[PMID: 9435889] |
| TE-671 | EC50 |
30 μM
Compound: 5, mecamylamine
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Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
Compound was evaluated for functional potencies and efficacies at human muscle type Nicotinic acetylcholine receptor in TE671 cells
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[PMID: 9435889] |
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.
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Cell Line:SCG neurons
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Concentration:10 μM
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Incubation Time:48 h
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Result:Reduced the nicotine-facilitated increase in ERK1/2.
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.
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Animal Model:Choroidal neovascularization (CNV) mice model[1]
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Dosage:50 mg/kg/day, 2 days
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Administration:Subcutaneous pumps implanted beneath the skin of the back, 200 μL and mean pumping rate of 0.5 μL/h.
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Result:Suppressed the development of CNV at Bruch’s membrane rupture sites in the absence of nicotine.
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Animal Model:C57BL/6J mice[5]
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Dosage:0.5-1 mg/kg
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Administration:Intraperitoneal injection
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Result:Had no effect in β2 knockout mice and α7 knockout mice, but decreased immobility time in wildtype littermates in the FST.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 60-40-2
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Appearance Solid
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Peso molecular 167.29
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Fòrmula C11H21N
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Color White to off-white
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SMILES
CC1(C)C(NC)(C)C2CCC1C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Plasticity in ventral pallidal cholinergic neuron-derived circuits contributes to comorbid chronic pain-like and depression-like behaviour in male mice. [Abstract]2023 Apr 17;14(1):2182. PMID: 37069246 -
Acta Pharmacol Sin
α4 nicotinic receptors on GABAergic neurons mediate a cholinergic analgesic circuit in the substantia nigra pars reticulata. [Abstract]2024 Jun;45(6):1160-1174. PMID: 38438581
Mecamylamine purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jun;45(6):1160-1174. [Abstract]
Injection of Mecamylamine hydrochloride (MEC) (100 μM; 300 nL) into the SNr of mice reduced both mechanical and thermal thresholds on both hind paws.
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Cell Biosci
Enhancing striatal acetylcholine facilitates dopamine release and striatal output in parkinsonian mice. [Abstract]2024 Dec 3;14(1):146. PMID: 39627827
Mecamylamine purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2024 Dec 3;14(1):146. [Abstract]
Mecamylamine hydrochloride (Meca) (50uM; 500 nL; i.c.) effectively decreased the power of Den-induced more DA release events in parkinsonian mice.
Mecamylamine purchased from MedChemExpress. Usage Cited in: Cell Biosci. 2024 Dec 3;14(1):146. [Abstract]
Mecamylamine hydrochloride (Meca) (3 mg/kg; i.p.) blocked the CNO-induced (5 mg/kg) increase in DA concentration in 6-OHDA-lesioned ChAT-Cre mice.
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Glia
Sustained Neuronal Stimulation Activates Paraventricular Thalamus Astrocytes for Chronicity of Neuropathic Pain in Mice. [Abstract]2026 Aug;74(8):e70183. PMID: 42231639 -
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Mecamylamine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Jul 6.
Mecamylamine hydrochloride (MEC) (1 mg/kg i.p.) blocked nAChRs and abolished the ACh-induced spine formation in ChAT-Cre × YFP-H mice.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[3]. Mahadevappa P Badanavalu, et al. Nicotine is neuroprotective to neonatal neurons of sympathetic ganglion in rat. Auton Neurosci. 2019 Jan;216:25-32. [Content Brief]
[4]. Katsuji Kiuchi, et al. Mecamylamine suppresses Basal and nicotine-stimulated choroidal neovascularization. Invest Ophthalmol Vis Sci. 2008 Apr;49(4):1705-11. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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