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).
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 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||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|
References are publications that support the biological activity of the product.
Seeman et al (1997) Atypical neuroleptics have low affinity for DA 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 DA 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
If you know of a relevant reference for Melperone hydrochloride, please let us know.
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Keywords: Melperone hydrochloride, Melperone hydrochloride supplier, 5-HT2A/D2, receptor, antagonists, neuroleptic, Serotonin, Receptors, Dopamine, D2, dopaminergic, 5-HT2A, 2495, Tocris Bioscience
1 Citation for Melperone hydrochloride
Citations are publications that use Tocris products. Selected citations for Melperone hydrochloride include:
Hacker et al (2015) Substrate-Dependent Inhibition of the Human Organic Cation Transporter OCT2: A Comparison of MetF. with Experimental Substrates. Brain Res 10 e0136451 PMID: 26327616
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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* or download 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.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.