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Anpirtoline hydrochloride (CAS 98330-05-3)

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Alternate Names:
2-Chloro-6-piperidin-4-ylsulfanylpyridine hydrochloride
Application:
Anpirtoline hydrochloride is a SR-1B agonist
CAS Number:
98330-05-3
Purity:
99%
Molecular Weight:
265.20
Molecular Formula:
C10H13ClN2S•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Anpirtoline hydrochloride is a selective agonist of SR-1B. Anpirtoline shows strong selectivity at SR-1B (Ki = 28 nM) over the SR-1A (Ki = 150 nM) and SR-2 (Ki = 1.49 μM) serotonin receptor subtypes. Anpirtoline is also described to produce antagonism at the SR-3 (Ki = 29.5 nM).


Anpirtoline hydrochloride (CAS 98330-05-3) References

  1. Regulation of striatal dopamine release through 5-HT1 and 5-HT2 receptors.  |  Ng, NK., et al. 1999. J Neurosci Res. 55: 600-7. PMID: 10082082
  2. Synthesis and analgesic activity of some condensed analogs of anpirtoline.  |  Rádl, S., et al. 1999. Arch Pharm (Weinheim). 332: 208-12. PMID: 10399490
  3. Enhanced 5-HT metabolism and synthesis rate by the new selective r5-HT1B receptor antagonist, NAS-181 in the rat brain.  |  Stenfors, C., et al. 2000. Neuropharmacology. 39: 553-60. PMID: 10728876
  4. Knockout mice reveal opposite roles for serotonin 1A and 1B receptors in prepulse inhibition.  |  Dulawa, SC., et al. 2000. Neuropsychopharmacology. 22: 650-9. PMID: 10788764
  5. Pharmacological characterisation of the decrease in 5-HT synthesis in the mouse brain evoked by the selective serotonin re-uptake inhibitor citalopram.  |  Stenfors, C., et al. 2001. Naunyn Schmiedebergs Arch Pharmacol. 363: 222-32. PMID: 11218075
  6. Oral drug self-administration in the home cage of mice: alcohol-heightened aggression and inhibition by the 5-HT1B agonist anpirtoline.  |  Miczek, KA. and de Almeida, RM. 2001. Psychopharmacology (Berl). 157: 421-9. PMID: 11605102
  7. Aggression escalated by social instigation or by discontinuation of reinforcement ('frustration') in mice: inhibition by anpirtoline: a 5-HT1B receptor agonist.  |  de Almeida, RM. and Miczek, KA. 2002. Neuropsychopharmacology. 27: 171-81. PMID: 12093591
  8. D-16949 (anpirtoline): a novel serotonergic (5-HT1B) psychotherapeutic agent assessed by its discriminative effects in the rat.  |  Swedberg, MD., et al. 1992. J Pharmacol Exp Ther. 263: 1015-22. PMID: 1335050
  9. Anpirtoline, a novel, highly potent 5-HT1B receptor agonist with antinociceptive/antidepressant-like actions in rodents.  |  Schlicker, E., et al. 1992. Br J Pharmacol. 105: 732-8. PMID: 1628159
  10. Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study.  |  Watanabe, A., et al. 2006. Nucl Med Biol. 33: 325-32. PMID: 16631081
  11. Hypothalamic neuropeptide Y (NPY) gene expression is not affected by central serotonin in the rainbow trout (Oncorhynchus mykiss).  |  Mancebo, MJ., et al. 2013. Comp Biochem Physiol A Mol Integr Physiol. 166: 186-90. PMID: 23752124
  12. The involvement of 5-HT-like receptors in the regulation of food intake in rainbow trout (Oncorhynchus mykiss).  |  Pérez Maceira, JJ., et al. 2014. Comp Biochem Physiol C Toxicol Pharmacol. 161: 1-6. PMID: 24365333
  13. 5-HT3 receptor antagonism by anpirtoline, a mixed 5-HT1 receptor agonist/5-HT3 receptor antagonist.  |  Göthert, M., et al. 1995. Br J Pharmacol. 114: 269-74. PMID: 7881726

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Anpirtoline hydrochloride, 5 mg

sc-201108
5 mg
$119.00

Anpirtoline hydrochloride, 25 mg

sc-201108A
25 mg
$453.00