Cerlapirdine
(Synonyms: SAM-531; PF-05212365) 目录号 : GC63961
Cerlapirdine (SAM-531, PF-05212365) 是一种选择性和有效的 5-羟色胺 6 (5-HT6) 受体的完全拮抗剂。Cerlapirdine 具有研究阿尔茨海默病的潜力。
Cas No.:925448-93-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer’s disease[1].
[1]. Tse S, et al. Disposition and metabolic profiling of [(14)C]cerlapirdine using accelerator mass spectrometry. Drug Metab Dispos. 2014;42(12):2023-2032.
Cas No. | 925448-93-7 | SDF | Download SDF |
别名 | SAM-531; PF-05212365 | ||
分子式 | C22H23N3O3S | 分子量 | 409.5 |
溶解度 | DMSO : 41.67 mg/mL (101.76 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
1 mM | 2.442 mL | 12.21 mL | 24.42 mL |
5 mM | 0.4884 mL | 2.442 mL | 4.884 mL |
10 mM | 0.2442 mL | 1.221 mL | 2.442 mL |
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Disposition and metabolic profiling of [(14)C]Cerlapirdine using accelerator mass spectrometry
Drug Metab Dispos 2014 Dec;42(12):2023-32.PMID:25217486DOI:10.1124/dmd.114.059675.
Cerlapirdine (SAM-531, PF-05212365) is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine and other 5-HT6 receptor antagonists have been in clinical development for the symptomatic treatment of Alzheimer's disease. A human absorption, distribution, metabolism, and excretion study was conducted to gain further understanding of the metabolism and disposition of Cerlapirdine. Because of the low amount of radioactivity administered, total (14)C content and metabolic profiles in plasma, urine, and feces were determined using accelerator mass spectrometry (AMS). After a single, oral 5-mg dose of [(14)C]Cerlapirdine (177 nCi), recovery of total (14)C was almost complete, with feces being the major route of elimination of the administered dose, whereas urinary excretion played a lesser role. The extent of absorption was estimated to be at least 70%. Metabolite profiling in pooled plasma samples showed that unchanged Cerlapirdine was the major drug-related component in circulation, representing 51% of total (14)C exposure in plasma. One metabolite (M1, desmethylcerlapirdine) was detected in plasma, and represented 9% of the total (14)C exposure. In vitro cytochrome P450 reaction phenotyping studies showed that M1 was formed primarily by CYP2C8 and CYP3A4. In pooled urine samples, three major drug-related peaks were detected, corresponding to cerlapirdine-N-oxide (M3), Cerlapirdine, and desmethylcerlapirdine. In feces, Cerlapirdine was the major (14)C component excreted, followed by desmethylcerlapirdine. The results of this study demonstrate that the use of the AMS technique enables comprehensive quantitative elucidation of the disposition and metabolic profiles of compounds administered at a low radioactive dose.