1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. nAChR
  3. Mecamylamine hydrochloride

Mecamylamine hydrochloride 

Cat. No.: HY-B1395 Purity: >98.0%
Handling Instructions

Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier.

For research use only. We do not sell to patients.

Mecamylamine hydrochloride Chemical Structure

Mecamylamine hydrochloride Chemical Structure

CAS No. : 826-39-1

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10 mg USD 210 Ask For Quote & Lead Time

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Description

Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].

IC50 & Target

nAChR[1]

In Vitro

Mecamylamine blocks muscle nAChRs in a use- and voltagedependent manner. Mecamylamine blocks the nicotinic currents via trapping mechanism. The main feature of this block is the phenomenon of block relief, which might be revealed by combined action of depolarization and activation of nAChRs. The experimental study of the Mecamylamine action on muscle nAChRs revealed that: (1) Mecamylamine (1-20 μM) reduces evoked end-plate currents (EPC) amplitude with Hill’s constant equal to 1.2 and IC50 = 7.8 μM at holding potential –70 mV; (2) the calculated depth of its interaction with the muscle nAChR channel is almost half of the one of neuronal nAChRs (0.37 compare to 0.72 for neuronal nAChRs); (3) simultaneous membrane depolarization and repetitive activation of postsynaptic nAChRs by motor nerve stimulation produced rapid block relief dependent on the degree of depolarization, number of conditioning signals and Mecamylamine concentration, and only slightly depended on the rate of stimulation[2].

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

In Vivo

Mecamylamine (0.5-1 mg/kg; Intraperitoneal injection; C57BL/6J mice) has antidepressant-like effects in both the TST and FST and these effects are dependent on bothβ2 andα7 subunits[3].

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

Animal Model: C57BL/6J mice (3-4 months) forced swim test (FST) and tail suspension test (TST)[3]
Dosage: 0.5 mg/kg, 0.75 mg/kg, 1 mg/kg
Administration: Intraperitoneal injection
Result: Significantly decreased immobility time in the TST at the 1.0-mg/kg dose but did not alter baseline locomotor activity. Also significantly decreased time immobile in the FST.
Clinical Trial
Molecular Weight

203.75

Formula

C₁₁H₂₂ClN

CAS No.

826-39-1

SMILES

CC1(C)C(NC)(C)C2CCC1C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 36.67 mg/mL (179.98 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9080 mL 24.5399 mL 49.0798 mL
5 mM 0.9816 mL 4.9080 mL 9.8160 mL
10 mM 0.4908 mL 2.4540 mL 4.9080 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (13.50 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (13.50 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (13.50 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MecamylaminenAChRNicotinic acetylcholine receptorsNeuropsychiatricorallyganglionichypertensionblood-brainbarriervoltagedependentantidepressant-likeInhibitorinhibitorinhibit

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Mecamylamine hydrochloride
Cat. No.:
HY-B1395
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