Niaprazine
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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Biological half-life | ~4.5 hours |
| Identifiers | |
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| Synonyms | CERM-1709 |
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| KEGG | |
| ECHA InfoCard | 100.044.014 |
| Chemical and physical data | |
| Formula | C20H25FN4O |
| Molar mass | 356.437 g/mol |
| 3D model (Jmol) | |
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Niaprazine (INN) (brand name Nopron) is a sedative-hypnotic drug of the phenylpiperazine group. It has been used in the treatment of sleep disturbances since the early 1970s in several European countries including France, Italy, and Luxembourg. It is commonly used with children and adolescents on account of its favorable safety and tolerability profile and lack of abuse potential.
Originally believed to act as an antihistamine and anticholinergic, niaprazine was later discovered to have low or no binding affinity for the H1 and mACh receptors (Ki = > 1 μM), and was instead found to act as a potent and selective 5-HT2A and α1-adrenergic receptor antagonist (Ki = 75 nM and 86 nM, respectively). It possesses low or no affinity for the 5-HT1A, 5-HT2B, D2, and β-adrenergic, as well as at SERT and VMAT (Ki = all > 1 μM), but it does have some affinity for the α2-adrenergic receptor (Ki = 730 nM), likely acting as an antagonist there as well.
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