[Low-affinity binding sites of glucocorticoid].
The low-affinity glucocorticoid binding sites (LAGS) with steroid specificity were demonstrated in hepatic cytosol, cerebral cytosol, and thymocytes of rat. The Kd of LAGS was 1-10 mumol.L-1 as estimated by Scatchard, pseudo-scatchard, and competitive analysis. The specific binding of dexamethasone 1-100 nmol.L-1 was roughly parallel with its inhibition of [3H]UdR incorporation in thymocytes of rat, and both were blocked by mifepristone (RU-486), the competitive antagonist of glucocorticoids. These results suggest that the pharmacological activity of glucocorticoid might be mediated at least partially by LAGS.
Le
Y Y
YY
Department of Pathophysiology, Second Military Medical University, Shanghai, China.
Qian
G Z
GZ
Sui
L M
LM
Gong
Q Z
QZ
Xu
R B
RB
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000166:cytology; D003600:Cytosol / Q000378:metabolism; D003907:Dexamethasone / Q000378:metabolism; D005260:Female; D005938:Glucocorticoids / Q000378:metabolism*; D008099:Liver / Q000166:cytology; D008297:Male; D015735:Mifepristone / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013950:Thymus Gland / Q000166:cytology; D014222:Triamcinolone Acetonide / Q000378:metabolism
D005938:Glucocorticoids; D015735:Mifepristone; D003907:Dexamethasone; D014222:Triamcinolone Acetonide