Home GPCR & G Protein Sigma Receptor agonist Cutamesine Dihydrochloride

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Cutamesine Dihydrochloride Sigma Receptor agonist

Cat.No.S2917

Cutamesine dihydrochloride (SA4503 dihydrochloride,AGY94806 dihydrochloride) is a potent Sigma-1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
Cutamesine Dihydrochloride Sigma Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 441.43

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Quality Control

Batch: S291701 Water]88 mg/mL]false]DMSO]22 mg/mL]false]Ethanol]11 mg/mL]false Purity: 99.84%
99.84

Solubility

In vitro
Batch:

Water : 88 mg/mL

DMSO : 22 mg/mL (49.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 11 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 441.43 Formula

C23H32N2O2.2HCl

 Storage (From the date of receipt)
CAS No. 165377-44-6 Download SDF Storage of Stock Solutions

Synonyms SA4503 dihydrochloride, AGY94806 dihydrochloride Smiles Cl.Cl.COC1=C(OC)C=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1

Mechanism of Action

Targets/IC50/Ki
Sigma-1 receptor
17.4 mM
In vitro

SA 4503 has weak binding affinities for sigma 1 adrenergic, dopamine D, serotonin (5-HT)1A, 5-HT2, histamine H, muscarinic M1, and muscarinic M2 receptors at a concentration of 10 μM. GTP weaks SA 4503-induced inhibition of (+)-[3H]pentazocine binding in rat brain membranes. SA 4503 inhibits specific (+)-[3H]pentazocine binding in a competitive manner.

In vivo

SA 4503 (0.03 mg/kg-1 mg/kg s.c.) attenuates the dizocilpine (0.15 mg/kg i.p.) and L-NAME (100 mg/kg i.p.)-induced memory deficits following a bell-shaped curve in both the Y-maze for spatial working memory and step-down type passive avoidance test in mice. Progesterone (2 mg/kg s.c.) blocks the SA 4503 effects in the dizocilpine- and L-NAME-amnesia models, in accordance with the purported neurosteroids/sigma1 receptors interaction. SA 4503 (100 nM-300 nM) increases the electrically evoked release of acetylcholine in hippocampal but not striatal slices of rats. Concentrations below 100 nM does not alter the electrically evoked release of acetylcholine in either brain area. SA 4503 (1 mg/kg i.p. bid) produces a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons in rats. SA 4503 (1 mg/kg i.p. repeat ) produces a significant increase in the number of spontaneously active VTA DA neurons. The repeated administration of SA 4503 produces a greater alteration of the firing pattern of spontaneously active VTA compared to SNC DA neurons. Repeated treatment with SA 4503 (0.3 mg/kg) ameliorates the behavioral deficits in olfactory bulbectomized rats resembling depression symptoms in the open-field test, sexual behavior test, and cued and contextual fear-conditioning test. SA 4503 displays advantages over desipramine in the sexual behavior test. SA 4503 also reverses the decrease in the protein expression of NMDA receptor subunit (NR)1, but not NR2A or NR2B, in the prefrontal cortex, hippocampus, and amygdala of olfactory bulbectomized rats.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10400891/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17556637/
  • [6] https://pubmed.ncbi.nlm.nih.gov/16463398/

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