| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Iprindole targets the serotonin and norepinephrine transporters, inhibiting their reuptake and increasing the concentrations of these neurotransmitters in the synaptic cleft. Unlike conventional TCAs, iprindole has only weak antimuscarinic and sedative effects. Its distinct pharmacological profile results in fewer sedative and cardiovascular side effects than classical TCAs. The compound also has weak antimuscarinic effects.
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| ln Vitro |
In vitro, Iprindole acts as a tricyclic antidepressant with a distinct pharmacological profile. Its activity is typically assessed by measuring its ability to inhibit the reuptake of serotonin and norepinephrine in synaptosomal preparations or cell lines expressing neurotransmitter transporters. The compound's weak antimuscarinic and sedative effects distinguish it from conventional TCAs. Standard in vitro assays include neurotransmitter uptake inhibition assays, receptor binding studies, and assessment of monoamine oxidase inhibition.
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| ln Vivo |
At 100 mg/kg intraperitoneal, iprindole inhibits the absorption of 5-HT and noradrenaline by less than 50%.
In vivo, Iprindole has been studied for its antidepressant efficacy with fewer sedative and cardiovascular side effects than classical TCAs. As a tricyclic antidepressant, it would be expected to produce antidepressant effects in animal models of depression, such as the forced swim test or tail suspension test. Its weak antimuscarinic effects suggest a more favorable side effect profile compared to other TCAs. However, comprehensive in vivo pharmacological studies are limited. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Iprindole can be evaluated using membrane preparations from tissues expressing serotonin or norepinephrine transporters. Radioligand binding displacement experiments are performed using suitable radiolabeled ligands such as [3H]-paroxetine for serotonin transporters or [3H]-nisoxetine for norepinephrine transporters. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ligand. IC50 values are calculated from displacement curves.
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| Cell Assay |
For in vitro cellular assays, cells expressing serotonin or norepinephrine transporters are cultured in appropriate media. For neurotransmitter uptake assays, cells are incubated with [3H]-serotonin or [3H]-norepinephrine in the presence or absence of various concentrations of Iprindole. The amount of radiolabeled neurotransmitter taken up by the cells is measured by scintillation counting. The reduction in uptake compared to control indicates transporter inhibition. IC50 values are calculated from dose-response curves. For receptor binding studies, cells expressing various receptor subtypes are used to assess the compound's selectivity profile.
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| Animal Protocol |
For in vivo animal studies, Iprindole can be administered to rodents via oral gavage or intraperitoneal injection. In models of depression (e.g., forced swim test, tail suspension test, or chronic mild stress model), behavioral responses are assessed following compound administration. In models of anxiety, the elevated plus maze or open field test may be used. In cardiovascular studies, heart rate and blood pressure are monitored to assess the compound's cardiovascular effects. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
Iprindole has a molecular weight of 284.44 and a molecular formula of C19H28N2. It is a tricyclic antidepressant with a distinct pharmacological profile compared to conventional TCAs. It has actions and uses similar to those of amitriptyline but with only weak antimuscarinic and sedative effects. The compound is categorized under the ATC code N06AA13. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of Iprindole includes potential adverse effects associated with tricyclic antidepressants, including dry mouth, constipation, blurred vision, urinary retention, and drowsiness. However, iprindole has fewer sedative and cardiovascular side effects than classical TCAs. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of cardiovascular and central nervous system effects.
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| References |
[1]. The pharmacology of iprindole, a new antidepressant. Psychopharmacologia. 1969;15(3):169-85.
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| Additional Infomation |
Iprindole belongs to the indole class of compounds. It is a tricyclic antidepressant with similar effects and uses to amitriptyline, but with weaker anticholinergic and sedative effects. (Excerpt from Martindale Pharmacopoeia, 30th edition, page 257)
Iprindole (CAS 5560-72-5) is a tricyclic antidepressant with a distinct pharmacological profile compared to conventional TCAs. It has actions and uses similar to those of amitriptyline but has only weak antimuscarinic and sedative effects. It has been studied for its antidepressant efficacy with fewer sedative and cardiovascular side effects than classical TCAs. It is categorized under the ATC code N06AA13. It is available for research purposes only. |
| Molecular Formula |
C19H28N2
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|---|---|
| Molecular Weight |
284.44
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| Exact Mass |
284.225
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| CAS # |
5560-72-5
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| PubChem CID |
21722
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| Appearance |
Off-white to light yellow oil
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| Density |
1.04g/cm3
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| Boiling Point |
435.4ºC at 760mmHg
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| Flash Point |
217.1ºC
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| Index of Refraction |
1.573
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| LogP |
4.252
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
21
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| Complexity |
315
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCCN1C2=C(CCCCCC2)C3=CC=CC=C31
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| InChi Key |
PLIGPBGDXASWPX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H28N2/c1-20(2)14-9-15-21-18-12-6-4-3-5-10-16(18)17-11-7-8-13-19(17)21/h7-8,11,13H,3-6,9-10,12,14-15H2,1-2H3
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| Chemical Name |
3-(6,7,8,9,10,11-hexahydrocycloocta[b]indol-5-yl)-N,N-dimethylpropan-1-amine
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| Synonyms |
Iprindole; 5560-72-5; Pramindole; Galatur; Prondol;
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 120 mg/mL (421.88 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 3 mg/mL (10.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 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: 3 mg/mL (10.55 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (10.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5157 mL | 17.5784 mL | 35.1568 mL | |
| 5 mM | 0.7031 mL | 3.5157 mL | 7.0314 mL | |
| 10 mM | 0.3516 mL | 1.7578 mL | 3.5157 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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