1. Neuronal Signaling
  2. Sigma Receptor
  3. Cutamesine

Cutamesine (SA4503) is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine has antidepressant effects.

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Cutamesine Chemical Structure

Cutamesine Chemical Structure

CAS No. : 165377-43-5

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Description

Cutamesine (SA4503) is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine has antidepressant effects[1][2].

IC50 & Target[1]

Sigma 1 Receptor

17.4 nM (IC50)

Sigma 2 Receptor

1784 nM (IC50)

In Vitro

Exposure of the neurons to H2O2 induced cell death, while pretreatment with Cutamesine inhibits neuronal cell death. Cutamesine also reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1[2].

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

In Vivo

In substantia nigra pars compacta (SNC) and ventral tegmental area (VTA) in anesthetized, male Sprague-Dawley rats, Cutamesine (0.01-1.28 mg/kg; iv) does not significantly alter the firing rate or pattern of spontaneously active dopamine (DA) neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of Cutamesine does not alter the number of spontaneously active SNC and VTA DA neurons[3].
A single injection of 1 mg/kg i.p. of Cutamesine produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively[3].
The repeated administration (one injection per day for 21 days) of 0.3 and 1 mg/kg i.p. of Cutamesine produced a significant increase in the number of spontaneously active VTA DA neurons[3].

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

Clinical Trial
Molecular Weight

368.51

Formula

C23H32N2O2

CAS No.
SMILES

COC1=CC=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1OC

Shipping

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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Cutamesine Related Classifications

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Product Name:
Cutamesine
Cat. No.:
HY-14813
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