Sch-44643(Sch-44643) - 药物靶点：H1 receptor x PAF receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

H1 receptor x PAF receptor

作用机制

H1 receptor拮抗剂(组胺H1受体拮抗剂)、PAF receptor拮抗剂(血小板活化因子受体拮抗剂)

治疗领域

免疫系统疾病呼吸系统疾病

在研适应症-

非在研适应症

哮喘

原研机构

Merck Sharp & Dohme Corp.

在研机构-

非在研机构

Merck Sharp & Dohme Corp.

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C25H22ClN3O2

InChIKeyGKSHSRPPQWZQCC-UHFFFAOYSA-N

CAS号133330-43-5

关联

100 项与 Sch-44643 相关的临床结果

登录后查看更多信息

100 项与 Sch-44643 相关的转化医学

登录后查看更多信息

100 项与 Sch-44643 相关的专利（医药）

登录后查看更多信息

1

项与 Sch-44643 相关的文献（医药）

1996-12-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

Determination of plasma concentrations of SCH 44643 by a GC method and correlation of plasma concentration and anti-PAF activity in cynomolgus monkeys

3区 · 医学

Article

作者: Hong-Ki Kim ; Mitchell Cayen ; Chin-Chung Lin ; Motasim Billah ; Helen Gilchrest ; John Anthes ; Robert Egan

Inhibiting the action of platelet-activating factor (PAF) is a new therapeutic approach for the treatment of allergic disorders. SCH 44643 is a new orally-active antagonist of response to both PAF and histamine. This study was done to determine plasma drug concentrations using a GC method and to compare them to ex-vivo anti-PAF activity in the plasma of cynomolgus monkeys following a single oral (12.5 mg kg-1) administration. The GC method involved organic solvent extraction of monkey plasma followed by a GC analysis in a RTX-1 capillary column with a nitrogen/phosphorus detector. The method showed good precision (RSD < 8%) and accuracy (bias < 9%) with a limit of quantitation of 20 ng ml-1. The plasma profiles of SCH 44643 concentration and anti-PAF activity were very similar in each of the six monkeys. There was an excellent correlation (r = 0.9003) between anti-PAF activity and plasma concentration of SCH 44643, suggesting that the anti-PAF activity in cynomolgus monkeys was primarily due to unchanged SCH 44643, rather than its potential metabolite(s).

100 项与 Sch-44643 相关的药物交易

登录后查看更多信息