Detection of binding activity and biologic effect of a novel alpha-melanocyte-stimulating hormone analogue / 药学学报
Acta Pharmaceutica Sinica
;
(12): 269-273, 2007.
Article
in Chinese
| WPRIM
| ID: wpr-281909
ABSTRACT
Binding activity and biologic effect of a novel alpha-melanocyte-stimulating hormone analogue were tested on cells transiently expressing the human melanocortin-1 (MC1), MC3, MC4, and MC5 receptors. The human MC1 and MC5 receptor genes were cloned into the expression vector pcDNA3. 1/ myc-his(-) B. The vectors were transferred to HEK-293 cells by the calcium phosphate method. Stable receptor populations were generated using G418 selection (900 microg x mL(-1)) for subsequent bioassay analysis. K(i) values of the novel alpha-MSH analogue for MC1, MC3, MC4, and MC5 receptors were obtained in competition with [125I]-NDP-MSH for binding studies. The cyclic AMP level was tested by using [3H]-cyclic AMP kit. It is showed that K(i) values of the novel alpha-MSH analogue for MC1, MC3, MC4, and MC5 receptors were (0.159 +/- 0.040), (35.430 +/- 6.743), (19.293 +/- 2.780) and (2.230 +/- 0.670) nmol L(-1), respectively. Its EC50 values for MC1, MC3, MC4, and MC5 receptors were (0.45 +/- 0.07), (7.80 +/- 0.65), (2.55 +/- 0.23) and (0.33 +/- 0.09) nmol L(-1), respectively. In these tests, the novel alpha-MSH analogue is a MC1R and MC5R selective agonist.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Plasmids
/
Radioligand Assay
/
Tritium
/
Binding, Competitive
/
Alpha-MSH
/
Molecular Sequence Data
/
Kinetics
/
Transfection
/
Cell Line
Type of study:
Diagnostic study
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2007
Type:
Article
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