Biological Activity
Atypical neuroleptic; 5-HT2A/D2 receptor antagonist (Ki values are 120 and 180 nM respectively). Causes an increase in dopamine levels in the medial prefrontal cortex (mPFC) and nucleus accumbens and an increase in ACh in the mPFC. Also binds adrenergic α1 and α2 receptors (Ki values are 180 and 150 nM respectively).
Compound Libraries
Melperone hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 299.81 |
| Formula | C16H22FNO.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1622-79-3 |
| PubChem ID | 15386 |
| InChI Key | MQHYXXIJLKFQGY-UHFFFAOYSA-N |
| Smiles | Cl.CC1CCN(CCCC(=O)C2=CC=C(F)C=C2)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 | 29.98 | 100 | |
| ethanol | 29.98 | 100 | |
| water | 29.98 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 299.81. 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 | 3.34 mL | 16.68 mL | 33.35 mL |
| 5 mM | 0.67 mL | 3.34 mL | 6.67 mL |
| 10 mM | 0.33 mL | 1.67 mL | 3.34 mL |
| 50 mM | 0.07 mL | 0.33 mL | 0.67 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Seeman et al (1997) Atypical neuroleptics have low affinity for dopamine D2 receptors or are selective for D4 receptors. Neuropsychopharmacology. 16 93 PMID: 9015795
Ichikawa et al (2002) Atypical antipsychotic drugs, quetiapine, iloperidone, and melperone, preferentially increase dopamine and acetylcholine release in rat medial prefrontal cortex: role of 5-HT1A receptor agonism. Brain Res. 956 349 PMID: 12445705
Uhr et al (2005) P-glycoprotein is a factor in the uptake of dextromethorphan, but not of melperone, into mouse brain: evidence for an overlap in substrate specificity between P-gp and CYP2D6. J.Psychopharmacol. 18 509 PMID:
Keywords: Melperone hydrochloride, supplier, 5-HT2A/D2, receptor, antagonists, neuroleptic, Serotonin, Receptors, Dopamine, D2, dopaminergic, 5-HT2A, Receptors, D2, Receptors, 5-HT2A, Receptors, Tocris Bioscience
