Comparative Study
[Changes in the ligand affinity of benzodiazepine receptors in the presence of 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP)]
[Article in
Russian]
- PMID: 3028530
Item in Clipboard
Comparative Study
[Changes in the ligand affinity of benzodiazepine receptors in the presence of 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP)]
[Article in
Russian]
Biull Eksp Biol Med.
1987 Feb.
Abstract
4,5,6,7-tetrahydroisoxazolo-(5,4-c-)pyridin-3-ol (THIP) in concentrations of 100-500 microM inhibited 3H-flunitrazepam (3H FNZ) binding to intact membranes at 0 degrees C in 25 mM TRIS-HCl buffer. The inhibition of 3H FNZ binding was due to the decrease in the affinity and Bmax of 3H FNZ binding. The affinity for benzodiazepines (e.g. BZ-receptor agonists) was reduced in the presence of THIP, whereas the affinity for BZ-receptor antagonists was unchanged. The value of THIP-induced shift was dependent on the molarity of TRIS-HCl buffer and the concentration of THIP. The results obtained suggest that THIP-induced shifts have a predictive value in the determination of pharmacological efficacy of BZ-receptor ligands.
Similar articles
-
Pharmacological subtypes of the gamma-aminobutyric acidA receptors defined by a gamma-aminobutyric acid analogue 4,5,6,7-tetrahydroisoxazolo[5,4-c] pyridin-3-ol and allosteric coupling: characterization using subunit-specific antibodies.Mol Pharmacol. 1995 Oct;48(4):666-75. Mol Pharmacol. 1995. PMID: 7476892
-
Induction of low-affinity GABAA receptors by the GABA-agonist THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol) in cultured rat cerebellar granule cells is prevented by inhibition of polyamine biosynthesis.J Neurosci Res. 1994 Dec 15;39(6):656-62. doi: 10.1002/jnr.490390605. J Neurosci Res. 1994. PMID: 7897701
-
Bicuculline-sensitive and insensitive effects of THIP on the binding of [3H]flunitrazepam.Neuropharmacology. 1987 Jul;26(7A):737-41. doi: 10.1016/0028-3908(87)90236-x. Neuropharmacology. 1987. PMID: 3627382
-
Antinociceptive effect of the GABAmimetic 4,5,6,7-tetrahydroisoxazolo [5, 4-c]pyridin-3-ol (THIP): chronic treatment increases alpha-2 adrenoceptors in the mouse brain.J Pharmacol Exp Ther. 1984 May;229(2):386-90. J Pharmacol Exp Ther. 1984. PMID: 6325663
-
Pharmacodynamic effects and possible therapeutic uses of THIP, a specific GABA-agonist.Pharm Weekbl Sci. 1982 Oct 22;4(5):145-53. doi: 10.1007/BF01959034. Pharm Weekbl Sci. 1982. PMID: 6292818 Review.