Lack of binding of acetaminophen to 5-HT receptor or uptake sites (or eleven other binding/uptake assays)

被引：46

作者：

Raffa, RB

Codd, EE

机构：

[1] Drug Discovery, R.W. Johnson Pharmaceutical Res. I., Spring House

[2] R-327, R.W. Johnson Pharmaceutical Res. I., Spring House, PA 19477-0776, Welsh and McKean Rds.

来源：

LIFE SCIENCES | 1996年 / 59卷 / 02期

关键词：

acetaminophen; paracetamol; analgesia; 5-HT receptors; receptor assays; uptake sites;

D O I：

10.1016/0024-3205(96)00273-1

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The mechanism of analgesic action of acetaminophen (paracetamol) remains unknown. However, a central component distinct from that of the NSAIDs (non-steroidal antiinflammatory drugs) seems likely. A recent report (NeuroReport 6:1546-1548, 1995) suggests the involvement of 5-HT3 receptors. In the present study, we measured the affinity of acetaminophen at 5-HT3, as well as 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2, 5-HT2C, 5-HT4, 5-HT6, 5-HT7 and eleven other receptor sites and at serotonin and norepinephrine reuptake sites. At 10 mu M, acetaminophen inhibited less than 10% specific radioligand binding at any site. These findings: (i) suggest that acetaminophen's effect on serotonergic pathways is indirect, and (ii) circumscribe acetaminophen's possible central analgesic mechanism(s).

引用

页码：PL37 / PL40

页数：4

共 28 条

[1] THE BETA-1-ADRENOCEPTOR AND BETA-2-ADRENOCEPTOR AFFINITY OF ATENOLOL AND METOPROLOL - A RECEPTOR-BINDING STUDY PERFORMED WITH DIFFERENT RADIOLIGANDS IN TISSUES FROM THE RAT, THE GUINEA-PIG AND MAN [J].