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Submit ReviewAnpirtoline hydrochloride
Description: Highly potent 5-HT1B agonist; also 5-HT3 antagonist
Chemical Name: 6-Chloro-2-[piperidinyl-4-thio]pyridine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for Anpirtoline hydrochloride
Anpirtoline hydrochloride is a highly potent 5-HT1B receptor agonist (Ki values are 28, 150 and 1490 nM at 5-HT1B, 5-HT1A and 5-HT2 receptors respectively). Decreases central serotonin synthesis and attenuates aggressive behavior in vivo. Also acts as an antagonist at 5-HT3 receptors (Ki = 29.5 nM) and is brain penetrant.
Compound Libraries for Anpirtoline hydrochloride
Anpirtoline hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Anpirtoline hydrochloride
| M. Wt | 265.2 |
| Formula | C10H13ClN2S.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 99201-87-3 |
| PubChem ID | 6917943 |
| InChI Key | GRXDJABVNGUGCW-UHFFFAOYSA-N |
| Smiles | Cl.ClC1=NC(SC2CCNCC2)=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Anpirtoline hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 | ||
| DMSO | 26.52 | 100 |
Preparing Stock Solutions for Anpirtoline hydrochloride
The following data is based on the product molecular weight 265.2. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.77 mL | 18.85 mL | 37.71 mL |
| 5 mM | 0.75 mL | 3.77 mL | 7.54 mL |
| 10 mM | 0.38 mL | 1.89 mL | 3.77 mL |
| 50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
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Product Datasheets for Anpirtoline hydrochloride
References for Anpirtoline hydrochloride
References are publications that support the biological activity of the product.
Almeida and Miczek (2002) Aggression escalates by social instigation or by discontinuation of reinforcement ("frustration") in mice: inhibition by anpirtoline: a 5-HT1B receptor agonist. Neuropsychopharmacology 27 171 PMID: 12093591
Göthert et al (1995) 5HT3 receptor antagonism by anpirtoline, a mixed 5HT1 receptor agonist/5HT3 receptor antagonist. Br.J.Pharmacol. 114 269 PMID: 7881726
Swedberg et al (1992) D-16949 (anpirtoline): a novel serotonergic (5-HT1B) psychotherapeutic agent assessed by its discriminative effect in the rat. J.Pharmacol.Exp.Ther. 263 1015 PMID: 1335050
Watanabe et al (2006) Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Nucl.Med.Biol. 33 325 PMID: 16631081
If you know of a relevant reference for Anpirtoline hydrochloride, please let us know.
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Keywords: Anpirtoline hydrochloride, Anpirtoline hydrochloride supplier, potent, 5-HT1B, agonists, 5-HT3, antagonists, Serotonin, Receptors, 0703, Tocris Bioscience
3 Citations for Anpirtoline hydrochloride
Citations are publications that use Tocris products. Selected citations for Anpirtoline hydrochloride include:
Gadgaard & Jensen (2020) Functional characterization of 5-HT1A and 5-HT1B serotonin receptor signaling through G-protein-activated inwardly rectifying K+ channels in a fluorescence-based membrane potential assay. Biochem Pharmacol 175 PMID: 32088264
Carvalho-Dias (2017) Serotonin regulates prostate growth through androgen receptor modulation. Sci Rep 7 15428 PMID: 29133842
Müller et al (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One 4 e6453 PMID: 19649285
Do you know of a great paper that uses Anpirtoline hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.