Convolamine hydrochloride
Convolamine hydrochloride is a tropane alkaloid and a potent Sigma-1 receptor positive allosteric modulator with an IC50 value of 289 nM. Convolamine hydrochloride can be extracted from Convolvulus plauricalis. Convolamine hydrochloride exhibits cognitive-improving and neuroprotective properties. Convolamine hydrochloride can be used in research related to Wolfram syndrome and Alzheimer's disease.
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- No. CAS: 5896-59-3
- Fòrmula: C17H24ClNO4
- Peso molecular:341.83
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Sigma 1 Receptor 289 nM (IC50) |
Sigma 2 Receptor 13 μM (IC50) |
Convolamine (100 nM, 30 μM; 60-120 min) hydrochloride does not bind to the S1R agonist/antagonist binding site but has moderate affinity for S2R in Jurkat human leukemic T cell membranes, with an S2R IC50 of 13 μM[1].
Convolamine (0.1-30 μM; 30 min) hydrochloride acts as a positive modulator of S1R in GFP-S1R-oe CHO cells, with an IC50 of 289 nM for enhancing PRE-084-mediated S1R/BiP dissociation, but does not act as an S1R agonist on its own[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GFP-S1R-overexpressing CHO (GFP-S1R-oe CHO) cells
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Concentration:30 μM (single-compound testing); 0.1, 0.3, 1, 3, 10 μM (positive modulation testing)
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Incubation Time:30 min at 37°C
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Result:Failed to dissociate S1R from BiP at concentrations up to 30 μM, confirming it is not an S1R agonist.
Shifted the PRE-084 IC50 from 468 nM to lower values (484 nM at 0.1 μM, 269 nM at 0.3 μM, 206 nM at 1 μM, 146 nM at 3 μM, 158 nM at 10 μM) when co-administered with increasing concentrations of PRE-084.
Had an IC50 of 289 nM for its positive modulatory effect.
Convolamine (1 mg/kg; i.p.) hydrochloride reverses learning and memory impairments in Wfs1ΔExon8 mice, restoring their performance in multiple behavioral tests to wild-type levels[1].
Convolamine (0.1-3 mg/kg; i.p.; single administration) hydrochloride exerts an anti-amnesic effect on dizocilpine-induced learning impairment via σ-1 receptor-mediated activity, with the peak efficacy observed at 1 mg/kg[1].
Convolamine (0.3-3 mg/kg; intraperitoneal injection; single administration) hydrochloride exerts neuroprotective effects against Amyloid-β[25-35]-induced learning impairment in mice, with the optimal efficacy observed at the dose of 1 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wfs1abKO double-mutant line (5 days post-fertilization larvae); wfs1abWT wild-type line (5 days post-fertilization larvae)[1]
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Dosage:0.3 μM; 1 μM; 3 μM
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Administration:immersion; 24 hours
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Result:Dose-dependently abolished the hyperlocomotor response of wfs1abKO larvae without affecting basal locomotion in wfs1abWT larvae.
Co-treatment with 3 μM NE-100 attenuated convolamine's effect on wfs1abKO larvae (p = 0.07 vs. convolamine alone).
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Animal Model:Wfs1ΔExon8 (129S6/SvEvTac C57BL/6J background, 3 months old, male and female); Wfs1WT control littermates (3 months old, male and female)[1]
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Dosage:1 mg/kg
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Administration:i.p.; single dose
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Result:Significantly attenuated the deficit in spontaneous alternation in Wfs1ΔExon8 mice, bringing alternation percentages close to Wfs1WT levels.
Reversed the decreased step-through latency in passive avoidance and improved short-term memory index, latency to reach the platform location, and platform location crossings in the active avoidance probe test, with outcomes not significantly different from Wfs1WT controls.
Exploratory behavior (arm entries in Y-maze) was unaffected by treatment.
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Animal Model:Swiss CD-1 (RjOrl:SWISS, male, 7-9 weeks old)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently (bell-shaped curve) attenuated dizocilpine-induced deficits in spontaneous alternation in the Y-maze (significant at 0.1, 0.3, 1 mg/kg).
Reversed dizocilpine-induced decreases in step-through latency (significant at 1 mg/kg) and increases in escape latency (significant at 0.3, 1, 3 mg/kg) in passive avoidance.
Co-treatment with NE-100 blocked convolamine's effect on alternation and step-through latency.
Did not affect dizocilpine-induced hyperlocomotion in the Y-maze.
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Animal Model:Swiss CD-1 (RjOrl:SWISS, male, 7-9 weeks old)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.p.; single dose
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Result:At 0.3, 1, and 3 mg/kg significantly attenuated amyloid-β[25-35]-induced deficits in spontaneous alternation in the Y-maze.
At 1 mg/kg, restored a significant short-term memory index in active avoidance, improved latency to reach the platform location, and reversed the amyloid-β[25-35]-induced decrease in platform location crossings in the active avoidance probe test.
No significant effect was observed in passive avoidance.
Chemical Information
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No. CAS 5896-59-3
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Peso molecular 341.83
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Fòrmula C17H24ClNO4
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SMILES
O=C(C(C=C1)=CC(OC)=C1OC)O[C@H](C[C@]2([H])CC3)C[C@]3([H])N2C.Cl
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Structure Classification
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Initial Source
Chlamydia pneumoniae
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Convolamine hydrochloride Related Classifications
HY-N15339A Related Classifications
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