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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% (HPLC)
Biological Activity for PNU 142633
PNU 142633 is a 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.
Compound Libraries for PNU 142633
PNU 142633 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PNU 142633
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PNU 142633
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.25 | 100 |
Preparing Stock Solutions for PNU 142633
The following data is based on the product molecular weight 422.53. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for PNU 142633
References for PNU 142633
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for PNU 142633, please let us know.
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Keywords: PNU 142633, PNU 142633 supplier, selective, 5-HT1D, agonists, Serotonin, Receptors, PNU142633, 1985, Tocris Bioscience
Citations for PNU 142633
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.