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(+)-Igmesine hydrochloride

σ1 receptor ligand CAS# 130152-35-1

(+)-Igmesine hydrochloride

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Chemical structure

(+)-Igmesine hydrochloride

3D structure

Chemical Properties of (+)-Igmesine hydrochloride

Cas No. 130152-35-1 SDF Download SDF
PubChem ID 6438339 Appearance Powder
Formula C23H30ClN M.Wt 355.94
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name (E)-N-(cyclopropylmethyl)-N-methyl-3,6-diphenylhex-5-en-3-amine;hydrochloride
SMILES CCC(CC=CC1=CC=CC=C1)(C2=CC=CC=C2)N(C)CC3CC3.Cl
Standard InChIKey SCHQQPAJNUHKSV-RSGUCCNWSA-N
Standard InChI InChI=1S/C23H29N.ClH/c1-3-23(22-14-8-5-9-15-22,24(2)19-21-16-17-21)18-10-13-20-11-6-4-7-12-20;/h4-15,21H,3,16-19H2,1-2H3;1H/b13-10+;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of (+)-Igmesine hydrochloride

DescriptionSelective σ1 receptor ligand (KD = 19.1 nM), with little or no activity at σ2 receptors (IC50 > 1000 nM). Inhibits the NMDA-induced increase in cGMP in a concentration-dependent manner (IC50 value is approximately 100 nM). Weak inhibitor of brain 5-HT uptake in vitro. Exhibits neuroprotective and antidepressant effects.

(+)-Igmesine hydrochloride Dilution Calculator

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(+)-Igmesine hydrochloride Molarity Calculator

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Preparing Stock Solutions of (+)-Igmesine hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8095 mL 14.0473 mL 28.0946 mL 56.1892 mL 70.2366 mL
5 mM 0.5619 mL 2.8095 mL 5.6189 mL 11.2378 mL 14.0473 mL
10 mM 0.2809 mL 1.4047 mL 2.8095 mL 5.6189 mL 7.0237 mL
50 mM 0.0562 mL 0.2809 mL 0.5619 mL 1.1238 mL 1.4047 mL
100 mM 0.0281 mL 0.1405 mL 0.2809 mL 0.5619 mL 0.7024 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on (+)-Igmesine hydrochloride

IC50: 19.1 nM

JO 1784 is a selective σ1 receptor ligand.

The CNS σ receptor ligands, as is known, modulates central neurotransmitter systems ( noradrenergic-, glutaminergic-, and dopaminergic-neurons was included).

In vitro: Compared with control, data obtained displayed significant reduction in the densities of β-adrenergic, but not σ1, 5-HT1A, and GABAB receptors in fluoxetine (18%), desipramine (DMI, 32%) and JO 1784 (20%)-treated groups. Tyrosine hydroxylase (TH) activity was significantly (30–32%) decreased in all treated groups. Further, fluoxetine and DMI excluding the JO 1784 -treated groups diaplayed 85 and 40% reductions in serotonin (5-HT) and noradrenaline (NE) neuronal uptake, respectively. Following acute treatment, JO 1784 is inactive for monoamine oxidase (MAO) A or B [1].

In vivo: In vivo studies, JO 1784 at behaviorally active doses exhibited weak effects on the NE uptake but has no activity in altering 5-HT and DA synthesis or antagonizing selective drug-stimulated depletion of monoamine neuronal uptake. NMDA-induced potentiates cGMP was inhibited by JO 1784, indicating that JO 1784 may interfere with the NMDA receptor/NOS/cGMP pathway. Although it appears that the pharmacological actions of JO 1784 partially is modulated by the monoaminergic system, there is still need to find other possible mechanisms of antidepressant action [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1].  Akunne HC, Zoski KT, Whetzel SZ, Cordon JJ, Brandon RM, Roman F, Pugsley TA. Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant. Neuropharmacology. 2001 Jul;41(1):138-49.

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References on (+)-Igmesine hydrochloride

The sigma receptor ligand JO 1784 (igmesine hydrochloride) is neuroprotective in the gerbil model of global cerebral ischaemia.[Pubmed:7498313]

Eur J Pharmacol. 1995 Sep 5;283(1-3):217-25.

To assess the effects of the novel sigma receptor ligand JO 1784 ((+)-N-cyclopropyl-methyl-N-methyl-1,4-diphenyl-1-yl-but-3-en-1-ylami ne, hydrochloride or igmesine hydrochloride) on behavioural and histological changes following cerebral ischaemia, the gerbil model of cerebral ischaemia was used. Two experiments were carried out. In the first animals were either sham operated, subjected to 5 min of bilateral carotid occlusion or administered JO 1784 (25, 50, 75 or 100 mg/kg p.o.) 1, 24 and 48 h after 5 min bilateral carotid occlusion and histological evaluation carried out 96 h after surgery. In the second experiment the effects of JO 1784 administered at a dose of 100 mg/kg i.p. 30 min, 6, 24 and 48 h post-surgery on home cage activity and nitric oxide (NO) synthase activity in the cortex, hippocampus, cerebellum and brain stem 4 days after surgery was examined. Extensive neuronal death was observed in the CA1 region of 5 min occluded animals. JO 1784 (50, 75 and 100 mg/kg) provided significant protection against this ischaemia-induced cell death (P < 0.03-0.005). In the second experiment a large increase in home cage activity was observed for 5 min occluded animals for 12 h after surgery (P = 0.0018-0.02). A large increase in NO synthase activity was observed in all brain regions for 5 min occluded animals. Post-administration of JO 1784 attenuated the ischaemia-induced hyperactivity and increased NO synthase activities.(ABSTRACT TRUNCATED AT 250 WORDS)

Neuropharmacological profile of a selective sigma ligand, igmesine: a potential antidepressant.[Pubmed:11445194]

Neuropharmacology. 2001 Jul;41(1):138-49.

Igmesine is a selective sigma (sigma(1)) ligand that was reported to exert antidepressant action through an unknown mechanism of action. A number of neurochemical measures were taken in this study in efforts to understand its mode of action. Following 21-day drug treatments, the actions of igmesine on a number of neurochemical measures were investigated. Data obtained showed significant decreases in the densities of beta-adrenergic but not 5-HT(1A), sigma(1) and GABA(B) receptors in fluoxetine (18%), desipramine (DMI, 32%) and igmesine (20%)-treated groups when compared with control. Tyrosine hydroxylase (TH) activity was significantly (30-32%) reduced in all treated groups. Further, fluoxetine and DMI excluding the igmesine-treated groups showed 85 and 40% reductions in serotonin (5-HT) and noradrenaline (NE) neuronal uptake, respectively. Following acute treatment, igmesine lacked activity for monoamine oxidase (MAO) A or B (IC(50)>10 microM). In in vivo studies, at behaviorally active doses, igmesine showed weak effects on the NE uptake but lacked activity in altering 5-HT and DA synthesis or antagonizing selective drug-induced depletion of monoamine neuronal uptake. N-methyl-D-aspartate (NMDA)-induced increases in cGMP was blocked by igmesine indicating that igmesine may interfere with the NMDA receptor/nitric oxide synthase/cGMP pathway. Although it appears that part of the pharmacological actions of igmesine is mediated by the monoaminergic system, there is still need to explore other possible mechanisms of antidepressant action.

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