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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5 mg USD 123 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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

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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.

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Keywords:

MecamylaminenAChRNicotinic acetylcholine receptorsNeuropsychiatricorallyganglionichypertensionblood-brainbarriervoltagedependentantidepressant-likeInhibitorinhibitorinhibit

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Mecamylamine hydrochloride
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