2. Neuronal Signaling Immunology/Inflammation
  3. Sigma Receptor NO Synthase
  4. (+)-Igmesine hydrochloride

(+)-Igmesine hydrochloride  (Synonyms: JO1784)

Cat. No.: HY-108515 Purity: 99.0%
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(+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ1 receptor ligand with an IC50 of 39 nM. (+)-Igmesine hydrochloride binds σ1 receptors to activate G-proteins and modulate Ca2+ uptake. (+)-Igmesine (hydrochloride) attenuates ischaemia-induced nitric oxide synthase activity and hyperactivity. (+)-Igmesine hydrochloride can be used for the research of duodenal ulcers, gastric ulcers, and cerebral ischaemia.

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

(+)-Igmesine hydrochloride

(+)-Igmesine hydrochloride Chemical Structure

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Based on 1 publication(s) in Google Scholar

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(+)-Igmesine hydrochloride Related Antibodies

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Description

(+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ1 receptor ligand with an IC50 of 39 nM. (+)-Igmesine hydrochloride binds σ1 receptors to activate G-proteins and modulate Ca2+ uptake. (+)-Igmesine (hydrochloride) attenuates ischaemia-induced nitric oxide synthase activity and hyperactivity. (+)-Igmesine hydrochloride can be used for the research of duodenal ulcers, gastric ulcers, and cerebral ischaemia[1][2][3][4].

IC50 & Target[1]

σ1

39 nM (IC50)

In Vitro

(+)-Igmesine (1 nM-10 μM; 52 h) hydrochloride potently suppresses Phytohemagglutinin-P (HY-N7038A)-, Concanavalin A (HY-P2149)-, and pokeweed mitogen-stimulated proliferation of rat lymphocytes with reductions in tritiated thymidine uptake[4].
(+)-Igmesine (1 nM-10 μM; 40 min-52 h) hydrochloride exhibits dose-dependent suppression of rat neutrophil phagocytosis and mitogen-stimulated rat lymphocyte proliferation[4].

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

(+)-Igmesine hydrochloride Related Antibodies

Cell Proliferation Assay[4]

Cell Line: rat lymphocytes
Concentration: 1 nM; 100 nM; 10 μM
Incubation Time: 52 h
Result: Potently suppressed Phytohemagglutinin-P -, Concanavalin A-, and pokeweed mitogen-stimulated proliferation of rat lymphocytes with reductions in tritiated thymidine uptake.
In Vivo

(+)-Igmesine (1-10 mg/kg; p.o.; single dose) hydrochloride potently protects rats from cysteamine-induced duodenal ulcers, with an ED50 of 4.14 mg/kg p.o. and a 71% reduction in ulcer index at 10 mg/kg p.o[1].
(+)-Igmesine (p.o.; single dose) hydrochloride weakly protects rats from multiple models of gastric mucosal damage, with ED50 values ranging from 25.2 to 55.4 mg/kg p.o[1].
(+)-Igmesine (1-30 mg/kg; i.d.; single dose) hydrochloride does not exhibit gastric antisecretory activity in pylorus-ligated rats[1].
(+)-Igmesine (0.25-2 mg/kg; i.v.; single bolus) hydrochloride dose-dependently stimulates duodenal bicarbonate secretion in anesthetized rat[1].
(+)-Igmesine (25-100 mg/kg; p.o.; at 1, 24, and 48 hours post-surgery) hydrochloride provides statistically significant neuroprotection against ischaemia-induced hippocampal CA1 neuronal death in gerbils[2].
(+)-Igmesine (100 mg/kg; i.p.; at 30 minutes, 6, 24, and 48 hours post-surgery) hydrochloride significantly attenuates ischaemia-induced hyperactivity and increases in NO synthase activity in the hippocampus and brain stem of gerbils[2].

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

Animal Model: Sprague-Dawley (male, 180-220 g, cysteamine-induced duodenal ulcer)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Induced a dose-related decrease in ulcer index, with an ED50 of 4.14 mg/kg p.o.
Reduced the mean ulcer index from 33.2 mm2 to 9.7 mm2, a 71% reduction, at 10 mg/kg p.o.
Lost protective effect when pre-treated with haloperidol (1 or 3 mg/kg s.c.), BMY 14,802 (10 mg/kg p.o.), or devazepide (30 mg/kg p.o.).
Animal Model: Sprague-Dawley (male, 250-400 g, pylorus-ligated Shay rat preparation)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.d.; single dose
Result: Did not significantly modify free or total gastric acid concentration or output at any tested dose compared to control rats.
Animal Model: Sprague-Dawley (male, 250-400 g, anesthetized in situ duodenal perfusion model)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1 mg/kg; 2 mg/kg
Administration: i.v.; single bolus
Result: Induced a dose-related increase in duodenal bicarbonate output, with a threshold dose of 0.25 mg/kg i.v. and maximal response at 1 mg/kg i.v.
Increased bicarbonate output from a basal 7.60 μEq·cm-1·h-1 to a plateau of 14.8 μEq·cm-1·h-1 (P < 0.001) that lasted 2 hours at 1 mg/kg i.v.
Did not further increase secretion when dose was doubled to 2 mg/kg i.v.
Lost stimulatory effect when pre-treated with haloperidol (0.50 mg/kg i.v.), BMY 14,802 (5 mg/kg i.v.), hexamethonium (1 mg/kg i.v.), tetrodotoxin (5 μg/kg i.v.), devazepide (0.50 mg/kg i.v.), or bilateral truncal vagotomy.
Showed no significant change in stimulatory effect with atropine (0.25 mg/kg i.v.), SCH 23,390 (0.50 mg/kg i.v.), sulpiride (1 mg/kg i.v.), prazosin (0.50 mg/kg i.v.), yohimbine (2 mg/kg i.v.), naloxone (0.20 mg/kg i.v.), indomethacin (0.25 mg/kg i.v.), or intracerebroventricular devazepide (17 μg/rat).
Animal Model: Male Mongolian gerbils (at least 3 months old, weighing >60 g, 5-minute bilateral carotid occlusion surgery)[2]
Dosage: 25 mg/kg; 50 mg/kg; 75 mg/kg; 100 mg/kg
Administration: p.o.; at 1, 24, and 48 hours post-surgery
Result: Provided partial neuroprotection against ischaemia-induced CA1 neuronal death at 25 mg/kg.
Provided significant neuroprotection against ischaemia-induced CA1 neuronal death (P < 0.03) at 50 mg/kg.
Provided significant neuroprotection against ischaemia-induced CA1 neuronal death (P < 0.01) at 75 mg/kg.
Provided significant neuroprotection against ischaemia-induced CA1 neuronal death (P < 0.005) at 100 mg/kg.
Animal Model: Male Mongolian gerbils (at least 3 months old, weighing >60 g, 5-minute bilateral carotid occlusion surgery)[2]
Dosage: 100 mg/kg
Administration: i.p.; at 30 minutes, 6, 24, and 48 hours post-surgery
Result: Attenuated ischaemia-induced hyperactivity (statistically significant at P < 0.0018 to 0.02) observed between 2-7 hours post-occlusion.
Attenuated ischaemia-induced increases in NO synthase activity across multiple brain regions, with statistically significant attenuation in the hippocampus (P < 0.03) and brain stem (P < 0.05).
Molecular Weight

355.94

Formula

C23H30ClN
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.CN(CC1CC1)[C@@](C/C=C/C2=CC=CC=C2)(CC)C3=CC=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 17.79 mg/mL (49.98 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8095 mL 14.0473 mL 28.0946 mL
5 mM 0.5619 mL 2.8095 mL 5.6189 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8095 mL 14.0473 mL 28.0946 mL 70.2366 mL
5 mM 0.5619 mL 2.8095 mL 5.6189 mL 14.0473 mL
10 mM 0.2809 mL 1.4047 mL 2.8095 mL 7.0237 mL
15 mM 0.1873 mL 0.9365 mL 1.8730 mL 4.6824 mL
20 mM 0.1405 mL 0.7024 mL 1.4047 mL 3.5118 mL
25 mM 0.1124 mL 0.5619 mL 1.1238 mL 2.8095 mL
30 mM 0.0936 mL 0.4682 mL 0.9365 mL 2.3412 mL
40 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7559 mL
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(+)-Igmesine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(+)-IgmesineJO1784JO 1784JO-1784Sigma ReceptorNO SynthaseNitric oxide synthasesNOSG-proteinsacetylcholineneutrophil phagocytosisnitric oxide synthaseσ1 receptorcerebral ischaemiaCa2+CCK-A receptorslymphocyte proliferationduodenal ulcersInhibitorinhibitorinhibit

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