Establishment of M1 Receptor Screening Model for Drugs for Alzheimer's Disease Using Radioimmunoassay Method
- VernacularTitle:应用放射性免疫方法建立抗早老性痴呆药的M1受体筛选模型
- Author:
Luyong ZHANG
;
Zhengzhou JIANG
;
Zhaohui CAI
;
Xiaochen ZHAO
;
Ming YAN
;
Xinyan LI
- Publication Type:Journal Article
- Keywords:
M1 receptor;
Alzheimer's disease;
cAMP;
drug screening
- From:
Journal of China Pharmaceutical University
2003;(1):41-45
- CountryChina
- Language:Chinese
-
Abstract:
AIM:To establish a screening model based on muscarinic receptor type 1(M1) for drugs against Alzheimer's disease (AD). METHOD: Human M1 receptor was expressed in HEK293 (human embryonic kidney) cells, and its activation was measured by the intracellular cAMP (cyclic AMP) level. Exogeneous 3H-cAMP was used to compete the intracellular cAMP binding sites. Acetylcholine chloride was used as a positive drug to ensure the sensitivity of this model. RESULT: HEK293 cell expressing system of human M1 receptor was established. Different concentrations of acetylcholine chloride (10-9～10-4 mol/L) activation of M1 receptor leads to an increase of intracellular cAMP 10.343×10-4～33.754×10-4 pmol/μl. CONCLUTION:This screening model has positive response to M1 receptor agonist and can be used for drug screening.
