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