PNU 142633

Catalog # Availability Size / Price Qty
1985/10
PNU 142633 | CAS No. 187665-65-2 | 5-HT1D Receptor Agonists
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Description: Highly selective 5-HT1D agonist

Chemical Name: (1S)-1-[2-[4-[4-(Aminocarbonyl)phenyl]-1-piperazinyl]ethyl]-3,4-dihydro-N-methyl-1H-2-benzopyran-6-carboxamide

Purity: ≥98%

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Biological Activity

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

Technical Data

M.Wt:
422.53
Formula:
C24H30N4O3
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
187665-65-2

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

  1. Preclinical studies characterizing the anti-migraine and cardiovascular effects of the selective 5-HT1D receptor agonist PNU-142633.
    McCall et al.
    Cephalalgia, 2002;22:799
  2. 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.
    Sanchez-Lopez et al.
    Br.J.Pharmacol., 2003;140:725
  3. Bovine isolated middle cerebral artery contractions to antimigraine drugs.
    Roon et al.
    Naunyn-Schmied.Arch.Pharmacol., 1999;360:591

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