Anpirtoline hydrochloride

Catalog #: 0703
3 Citations Datasheet / COA / SDS

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Anpirtoline hydrochloride | CAS No. 99201-87-3 | 5-HT1B Receptor Agonists

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Description: Highly potent 5-HT1B agonist; also 5-HT3 antagonist

Chemical Name: 6-Chloro-2-[piperidinyl-4-thio]pyridine hydrochloride

Purity: ≥99%

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Product Details

Citations (3)

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Biological Activity

Anpirtoline hydrochloride is a highly potent 5-HT_1B receptor agonist (K_i values are 28, 150 and 1490 nM at 5-HT_1B, 5-HT_1A and 5-HT₂ receptors respectively). Decreases central serotonin synthesis and attenuates aggressive behavior in vivo. Also acts as an antagonist at 5-HT₃ receptors (K_i = 29.5 nM) and is brain penetrant.

Technical Data

M.Wt:

265.2

Formula:

C₁₀H₁₃ClN₂S.HCl

Solubility:

Soluble to 100 mM in water and to 100 mM in DMSO

Purity:

≥99%

Storage:

Desiccate at +4°C

CAS No:

99201-87-3

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.

Background References

High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
Aggression escalates by social instigation or by discontinuation of reinforcement ("frustration") in mice: inhibition by anpirtoline: a 5-HT_1B receptor agonist.
Almeida and Miczek
Neuropsychopharmacology, 2002;27:171
5HT₃ receptor antagonism by anpirtoline, a mixed 5HT₁ receptor agonist/5HT₃ receptor antagonist.
G?thert et al.
Br.J.Pharmacol., 1995;114:269
D-16949 (anpirtoline): a novel serotonergic (5-HT_1B) psychotherapeutic agent assessed by its discriminative effect in the rat.
Swedberg et al.
J.Pharmacol.Exp.Ther., 1992;263:1015
Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study.
Watanabe et al.
Nucl.Med.Biol., 2006;33:325

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Citations for Anpirtoline hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for Anpirtoline hydrochloride include:

3 Citations: Showing 1 - 3

Functional characterization of 5-HT_1A and 5-HT_1B serotonin receptor signaling through G-protein-activated inwardly rectifying K⁺ channels in a fluorescence-based membrane potential assay.
Authors: Gadgaard & Jensen
Biochem Pharmacol 2020;175
Serotonin regulates prostate growth through androgen receptor modulation.
Authors: Carvalho-Dias
Sci Rep 2017;7(1):15428
5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo.
Authors: Müller Et al.
PLoS One 2009;4:e6453

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