Date published: 2025-10-9

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PNU 142633 (CAS 187665-65-2)

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Alternate Names:
(1S)-1-[2-[4-[4-(Aminocarbonyl)phenyl]-1-piperazinyl]ethyl]-3,4-dihydro-N-methyl-1H-2-benzopyran-6-carboxamide
Application:
PNU 142633 is a high affinity SR-1D agonist
CAS Number:
187665-65-2
Purity:
≥98%
Molecular Weight:
422.53
Molecular Formula:
C24H30N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Very selective, high affinity 5-HT1D receptor agonist (Ki values are 6 and > 18000 nM at human 5-HT1D and 5-HT1B receptors respectively). Blocks neurogenic plasma protein extravasation and inhibits sympathetically-induced tachycardic responses in vivo.


PNU 142633 (CAS 187665-65-2) References

  1. The GR127935-sensitive 5-HT(1) receptors mediating canine internal carotid vasoconstriction: resemblance to the 5-HT(1B), but not to the 5-HT(1D) or 5-ht(1F), receptor subtype.  |  Centurión, D., et al. 2001. Br J Pharmacol. 132: 991-8. PMID: 11226129
  2. The anti-migraine 5-HT(1B/1D) agonist rizatriptan inhibits neurogenic dural vasodilation in anaesthetized guinea-pigs.  |  Williamson, DJ., et al. 2001. Br J Pharmacol. 133: 1029-34. PMID: 11487512
  3. Preclinical studies characterizing the anti-migraine and cardiovascular effects of the selective 5-HT1D receptor agonist PNU-142633.  |  McCall, RB., et al. 2002. Cephalalgia. 22: 799-806. PMID: 12485205
  4. Pharmacological profile of the 5-HT-induced inhibition of cardioaccelerator sympathetic outflow in pithed rats: correlation with 5-HT1 and putative 5-ht5A/5B receptors.  |  Sánchez-Lopez, A., et al. 2003. Br J Pharmacol. 140: 725-35. PMID: 14504136
  5. Further characterization of the 5-HT1 receptors mediating cardiac sympatho-inhibition in pithed rats: pharmacological correlation with the 5-HT1B and 5-HT1D subtypes.  |  Sánchez-López, A., et al. 2004. Naunyn Schmiedebergs Arch Pharmacol. 369: 220-7. PMID: 14673512
  6. Donitriptan, but not sumatriptan, inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors.  |  Muñoz-Islas, E., et al. 2006. Br J Pharmacol. 149: 82-91. PMID: 16880765
  7. Spinal sumatriptan inhibits capsaicin-induced canine external carotid vasodilatation via 5-HT1B rather than 5-HT1D receptors.  |  Muñoz-Islas, E., et al. 2009. Eur J Pharmacol. 615: 133-8. PMID: 19460365
  8. The 5-HT(1) receptors inhibiting the rat vasodepressor sensory CGRPergic outflow: further involvement of 5-HT(1F), but not 5-HT(1A) or 5-HT(1D), subtypes.  |  González-Hernández, A., et al. 2011. Eur J Pharmacol. 659: 233-43. PMID: 21473863
  9. mRNA expression of 5-hydroxytryptamine 1B, 1D, and 1F receptors and their role in controlling the release of calcitonin gene-related peptide in the rat trigeminovascular system.  |  Amrutkar, DV., et al. 2012. Pain. 153: 830-838. PMID: 22305629
  10. Chronic 5-HT2 receptor blockade unmasks the role of 5-HT1F receptors in the inhibition of rat cardioaccelerator sympathetic outflow.  |  García-Pedraza, JÁ., et al. 2018. Can J Physiol Pharmacol. 96: 328-336. PMID: 28886249
  11. Effect of a 5-HT1D receptor agonist on the reinstatement phase of the conditioned place preference test and hippocampal long-term potentiation in methamphetamine-treated rats.  |  Shahidi, S., et al. 2018. Brain Res. 1698: 151-160. PMID: 30076792
  12. Role of peripheral 5-HT5A receptors in 5-HT-induced cardiac sympatho-inhibition in type 1 diabetic rats.  |  García-Pedraza, JÁ., et al. 2020. Sci Rep. 10: 19358. PMID: 33168874
  13. The role of hippocampal 5-HT1D and 5-HT1F receptors on learning and memory in rats.  |  Afshar, S., et al. 2023. Naunyn Schmiedebergs Arch Pharmacol.. PMID: 36749399

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

PNU 142633, 10 mg

sc-204204
10 mg
$209.00