
Biological Activity
Selective 5-HT2B/2C receptor antagonist with low affinity for 5-HT1A receptors. Inhibits [3H]-mesulergine binding to 5-HT2C receptors with a pKD of 7.8. Inhibits 5-HT2B mediated responses in the rat fundus (pKB = 7.34).
Licensing Information
Sold with the permission of Novartis Pharma AG
Technical Data
M. Wt | 344.41 |
Formula | C15H20N2.C4H4O4 |
Storage | Store at RT |
CAS Number | 1417343-80-6 |
PubChem ID | 45073480 |
InChI Key | DXUZZRDHJMOLTN-MRYVXRNOSA-N |
Smiles | C(C=CC(O[H])=O)(O[H])=O.[H][C@@]23[C@@](CCN(C3)C)([H])CN(CC4)C1=C4C=CC=C12 |
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
Solubility | Soluble to 100 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 344.41. 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 | 2.9 mL | 14.52 mL | 29.04 mL |
5 mM | 0.58 mL | 2.9 mL | 5.81 mL |
10 mM | 0.29 mL | 1.45 mL | 2.9 mL |
50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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References
References are publications that support the products' biological activity.
Kalkman et al (1998) Cataleptogenic effect of subtype selective 5-HT receptor antagonists in the rat. Eur.J.Pharmacol. 343 201 PMID: 9570468
Mora et al (1997) Role of 5-HT2A and 5-HT2C receptor subtypes in the two types of fear generated by the elevated T-maze. Pharmacol.Biochem.Behav. 58 1051 PMID: 9408213
Nozulak et al (1995) (+)-cis 4,5,7a,8,9,10,11,11a-Octahydro-7H-10-methylindolo[1,7-bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity. J.Med.Chem. 38 28 PMID: 7837236
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