| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Anpirtoline hydrochloride targets the 5-HT1B receptor, a subtype of serotonin receptor. It acts as a potent agonist with a Ki of 28 nM. It also has affinity for 5-HT1A (Ki = 150 nM) and 5-HT2 (Ki = 1.49 µM) receptors. By activating 5-HT1B receptors, it modulates serotonergic neurotransmission, which is involved in pain perception and mood regulation.
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| ln Vitro |
In vitro, anpirtoline hydrochloride acts as a 5-HT1B receptor agonist. It has Ki values of 28 nM for 5-HT1B, 150 nM for 5-HT1A, and 1.49 µM for 5-HT2 receptors. Its affinity and selectivity for these receptors have been characterized in radioligand binding assays. These activities confirm its profile as a 5-HT1B receptor agonist.
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| ln Vivo |
In vivo, anpirtoline hydrochloride exhibits antinociceptive and antidepressant-like actions in rodents. These effects are mediated through its activity at 5-HT1B receptors. Its ability to modulate pain and mood has been demonstrated in animal models. However, it is not approved for clinical use.
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| Enzyme Assay |
The in vitro receptor binding assay for anpirtoline hydrochloride typically involves radioligand displacement studies using membrane preparations from cells expressing 5-HT1B, 5-HT1A, and 5-HT2 receptors. The compound's affinity (Ki) is determined by measuring its ability to displace a specific radiolabeled ligand from these receptors. These cell-free assays provide a direct measure of the compound's binding profile.
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| Cell Assay |
In vitro cellular assays for anpirtoline hydrochloride assess its functional activity at 5-HT1B receptors. Cells expressing the 5-HT1B receptor are treated with anpirtoline, and downstream signaling, such as inhibition of cAMP accumulation, is measured. These assays demonstrate the compound's functional activity as an agonist at 5-HT1B receptors.
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| Animal Protocol |
In vivo animal studies for anpirtoline hydrochloride have been conducted in rodent models to evaluate its antinociceptive and antidepressant-like effects. These studies typically involve administering the compound to animals and measuring pain responses or behavioral changes. Its efficacy in these models supports its potential for studying serotonin-related disorders.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for anpirtoline hydrochloride are not extensively detailed in the available literature. As a small molecule, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as half-life and bioavailability are not provided. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for anpirtoline hydrochloride are not extensively detailed in the available literature. As a 5-HT1B receptor agonist, its toxicity profile is likely related to its mechanism of action. However, its antinociceptive and antidepressant-like effects in animal models suggest a manageable safety profile. It is intended for research purposes only.
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| References |
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| Additional Infomation |
See also: Ampitoline (note moved to).
Anpirtoline hydrochloride is a centrally acting 5-HT1B receptor agonist with Ki values of 28 nM for 5-HT1B, 150 nM for 5-HT1A, and 1.49 µM for 5-HT2 receptors. It has antinociceptive and antidepressant-like actions in rodents. It is a research compound for studying serotonin receptor pharmacology. It is not approved for clinical use. |
| Molecular Formula |
C10H13N2SCL.HCL
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|---|---|
| Molecular Weight |
265.20256
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| Exact Mass |
264.025
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| CAS # |
99201-87-3
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| Related CAS # |
Anpirtoline; 98330-05-3
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| PubChem CID |
6917943
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.709
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
174
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.ClC1N=C(SC2CCNCC2)C=CC=1
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| InChi Key |
GRXDJABVNGUGCW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H13ClN2S.ClH/c11-9-2-1-3-10(13-9)14-8-4-6-12-7-5-8;/h1-3,8,12H,4-7H2;1H
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| Chemical Name |
2-chloro-6-piperidin-4-ylsulfanylpyridine;hydrochloride
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: ~100 mg/mL (~377.1 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (9.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (9.43 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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7707 mL | 18.8537 mL | 37.7074 mL | |
| 5 mM | 0.7541 mL | 3.7707 mL | 7.5415 mL | |
| 10 mM | 0.3771 mL | 1.8854 mL | 3.7707 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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