PNU 142633

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Cat.No. 1985 - PNU 142633 | C24H30N4O3 | CAS No. 187665-65-2
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% (HPLC)
Datasheet
Citations
Literature

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 187665-65-2
PubChem ID 9845148
InChI Key PNTVCCRNJOGKGA-QFIPXVFZSA-N
Smiles O=C(NC)C3=CC(CCO2)=C(C=C3)[C@@H]2CCN1CCN(C4=CC=C(C(N)=O)C=C4)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.25 100

Preparing Stock Solutions

The following data is based on the product molecular weight 422.53. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.37 mL 11.83 mL 23.67 mL
5 mM 0.47 mL 2.37 mL 4.73 mL
10 mM 0.24 mL 1.18 mL 2.37 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID: 12485205

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 PMID: 14504136

Roon et al (1999) Bovine isolated middle cerebral artery contractions to antimigraine drugs. Naunyn-Schmied.Arch.Pharmacol. 360 591 PMID:


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Keywords: PNU 142633, supplier, selective, 5-HT1D, agonists, Serotonin, Receptors, PNU142633, 5-HT1D, Receptors, Tocris Bioscience

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GPCR

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5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

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