PNU 142633 is a very selective, high affinity SR-1D agonist (Ki values are 6 and > 18000 nM at human SR-1D and SR-1B, respectively). PNU 142633 blocks neurogenic plasma protein extravasation and inhibits sympathetically-induced tachycardic responses in vivo.
Roon et al (1999) Bovine isolated middle cerebral artery contractions to antimigraine drugs. Naunyn-Schmied.Arch.Pharmacol. 360 591. McCall et al (2002) Preclinical studies characterizing the anti-migraine and cardiovascular effects of the selective 5-HT1D receptor agonist PNU-142633. Cephalalgia 22 799. Sanchez-Lopez et al (2003) 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. Br.J.Pharmacol. 140 725.
Soluble in DMSO (100 mM), and ethanol (20 mM).
Store at 4° C
287.06° C (Predicted)
~652.5° C at 760 mmHg (Predicted)
~1.2 g/cm3 (Predicted)
n20D 1.60 (Predicted)
SR-1D: Ki= 4.6 nM (human)
pKb: 7.27 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Rated 5 out of
McCall et alMcCall et al. (PubMed ID 12485205) found that PNU 142633, a highly selective 5-HT1D receptor agonist, blocked plasma protein extravasation and reduced the increase in cat nucleus trigeminal caudalis blood flow caused by electrical stimulation of the trigeminal ganglion. -SCBT Publication Review
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