| 药品名称 | Tiapride |
|---|---|
| 分子靶点 | T-cell-specific surface glycoprotein CD28 |
| 药物类型 | Small Molecule |
| 研发阶段 | Investigational |
| 药物描述 | Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. |
| 结构式 |
 |
| 药物别名 | Thiapride;Tiaprida;Tiapride;Tiapridum |
| 治疗类别 | Acids, Carbocyclic;Amides;Amines;Antipsychotic Agents;Benzamides and benzamide derivatives;Benzene Derivatives;Benzoates;Central Nervous System Agents;Central Nervous System Depressants;Dopamine Agents;Dopamine Antagonists;Dopamine D2 Receptor Antagonists;Ethylamines;Nervous System;Neurotoxic agents;Neurotransmitter Agents;Psycholeptics;Psychotropic Drugs;Tranquilizing Agents |
| UNII号 | LAH70H9JPH |
| CAS号 | 51012-32-9 |
| 分子量 | 328.427 |
| 分子式 | C15H24N2O4S |
| 适应症 | Tiapride is indicated for the treatment of a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. |
| 药效学 | Tiapride has a high degree of regional selectivity for limbic areas. One study found that tiapride shows over three times as much affinity for limbic areas than striatal areas as opposed to the near equal selectivity for limbic and striatal regions shown by haloperidol.Another study in rats found tiapride's affinity for the septum, a limbic region, to be over thirty times as high as for the striatum.Efficacy at the D2 receptor is moderate, with 80 percent of receptors occupied even in the presence of excess tiapride concentrations. |
| 作用机制 | Tiapride is a selective dopamine D2 and D3 receptor antagonist, offering an advantage over other neuroleptic drugs, such as haloperidol and risperidone, which bind a range of targets including four of the five known dopamine receptor subtypes (D1-4), serotonin (5-HT2A, 2C), α1- and α2-adrenergic, and histamine H1 receptors. Compared to these drugs, tiapride has a relatively moderate affinity for its target receptors, displacing 50 percent of 3H-raclopride binding at a concentration of 320 nM at D2 receptors and a concentration of 180 nM at D3 receptors. |
| 吸收 | The bioavailability of tiapride is approximately 75 percent. It has a Tmax is 0.4-1.5 hours and Tss is 24-48 hours with 3 time daily dosing. Benzamide and its derivatives are highly water-soluble but known to cross the blood-brain barrier, necessitating carrier-mediated transport. |
| 分布量 | Tiapride distributes rapidly and exhibits virtually no binding to plasma proteins, giving it a relatively high volume of distribution |
| 蛋白结合 | Negligible |
| 代谢 | Tiapride is minimally metabolized in humans, 70 % of the drug is eliminated in unchanged form in the urine within 24 hours. Only low concentration of N-desethyl tiapride and tiapride N-oxide and no phase II metabolites were detected. |
| 排泄 | Urine (70% as unchanged tiapride) |
| 半衰期 | 2.9–3.6 hours |
| 清除 | 16.6 l/h. |
| ATC代码 | N05AL03 |
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