| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 100mg | |||
| Other Sizes |
| Targets |
- Isocorynoxeine exerts suppressive effects by targeting the 5-HT2A receptor in the brain [1]
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|---|---|
| ln Vitro |
Isocorynoxeine suppresses 5-HT currents mediated by 5-HT2A receptors. In the brain, isocorynoxeine prefers to interact with 5-HT2A receptors over 5-HT2C receptors. Compared to 5-HT2A receptors - oocyte-mediated responses, isocorynoxeine has less inhibitory effect (IC50 value > 100 μM) at 5-HT2C receptor-mediated responses. In Xenopus laevis oocytes expressing 5-HT2A receptors, isocorynoxeine reduces 5-HT-evoked currents in a dose-dependent and competitive manner; however, in oocytes expressing 5-HT2C receptors, the inhibitory action is less pronounced[1].
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| ln Vivo |
The effects of isostatin, leucine, and rhynchophylline (isotropin-related alkaloids) on 5-MeO-DMT-induced head twitching behavior in reserpine mice were investigated in Uncaria species. This behavior was not impacted by either corynoxeine [H=0.242, P=0.886] or rhynchophylline [H=1.369, P=0.504], but at 30 mg/kg (ip) [H=7.582, P<0.01][1], isocorynoxeine dramatically reduced the behavior.
- In behavioral studies, Isocorynoxeine (administered at specific doses) suppressed 5-HT2A receptor-mediated behaviors in experimental animals. It reduced the head-twitch response induced by a 5-HT2A receptor agonist, and attenuated hyperlocomotion associated with 5-HT2A receptor activation [1] - In electrophysiological studies, Isocorynoxeine modified the electrical activity of neurons in brain regions enriched with 5-HT2A receptors (e.g., prefrontal cortex). It decreased the frequency of spontaneous excitatory postsynaptic potentials (sEPSPs) in these neurons, indicating inhibition of 5-HT2A receptor-dependent synaptic transmission [1] |
| Enzyme Assay |
- Brain membrane preparations were isolated from experimental animals (e.g., rats) and incubated with a radioactive ligand specific for the 5-HT2A receptor, along with different concentrations of Isocorynoxeine. After incubation, unbound ligand was removed by filtration, and the radioactivity of the bound ligand was measured using a scintillation counter. The assay was used to determine the ability of Isocorynoxeine to compete with the radioactive ligand for binding to the 5-HT2A receptor [1]
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| Animal Protocol |
- Male rats (or mice, depending on the experiment) were randomly divided into control group, Isocorynoxeine treatment groups (with doses such as 1, 5, 10 mg/kg), and positive control group (treated with a known 5-HT2A receptor antagonist). Isocorynoxeine was dissolved in an appropriate solvent (e.g., saline with a small amount of DMSO) and administered via intraperitoneal injection 30 minutes before behavioral or electrophysiological tests [1]
- For behavioral tests: The head-twitch response was induced by subcutaneous injection of a 5-HT2A receptor agonist, and the number of head twitches was counted within 1 hour. Hyperlocomotion was evaluated by recording the total distance traveled by animals in an open field arena over 30 minutes [1] - For electrophysiological tests: Animals were anesthetized, and a glass microelectrode was inserted into the prefrontal cortex to record the electrical activity of individual neurons. The frequency and amplitude of sEPSPs were recorded for 10 minutes before and after administration of Isocorynoxeine to assess changes in synaptic transmission [1] |
| References | |
| Additional Infomation |
Isocorynoxeine has been reported in Uncaria sinensis, Mitragyna rotundifolia, and other organisms with relevant data. See also: Cat's Claw (partial). - Isocorynoxeine inhibits the function of 5-HT2A receptors in the brain by competitively binding to receptors, which may help explain its potential impact on neuropsychiatric disorders (such as schizophrenia and anxiety) associated with abnormal 5-HT2A receptor activity. Studies have confirmed that its inhibitory effect on 5-HT2A receptor function is specific because at the tested dose, it has no significant effect on other serotonin receptor subtypes (such as 5-HT1A and 5-HT3) [1]
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| Molecular Formula |
C22H26N2O4
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|---|---|
| Molecular Weight |
382.4528
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| Exact Mass |
382.189
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| CAS # |
51014-29-0
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| PubChem CID |
3037448
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
562.7±50.0 °C at 760 mmHg
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| Flash Point |
294.1±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.606
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| LogP |
3.07
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
690
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CO/C=C(\[C@H]1C[C@H]2[C@]3(CCN2C[C@@H]1C=C)C4=CC=CC=C4NC3=O)/C(=O)OC
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| InChi Key |
MUVGVMUWMAGNSY-VKCGGMIFSA-N
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| InChi Code |
InChI=1S/C22H26N2O4/c1-4-14-12-24-10-9-22(17-7-5-6-8-18(17)23-21(22)26)19(24)11-15(14)16(13-27-2)20(25)28-3/h4-8,13-15,19H,1,9-12H2,2-3H3,(H,23,26)/b16-13+/t14-,15-,19-,22-/m0/s1
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| Chemical Name |
methyl (E)-2-[(3S,6'R,7'S,8'aS)-6'-ethenyl-2-oxospiro[1H-indole-3,1'-3,5,6,7,8,8a-hexahydro-2H-indolizine]-7'-yl]-3-methoxyprop-2-enoate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~65.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6147 mL | 13.0736 mL | 26.1472 mL | |
| 5 mM | 0.5229 mL | 2.6147 mL | 5.2294 mL | |
| 10 mM | 0.2615 mL | 1.3074 mL | 2.6147 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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