TY - JOUR
T1 - Differential discrimination of G-protein coupling of serotonin(1A) receptors from bovine hippocampus by an agonist and an antagonist
AU - Harikumar, K. G.
AU - Chattopadhyay, Amitabha
N1 - Funding Information:
This work was supported by a Grant (BT/R and D/9/5/93) to A.C. from the Department of Biotechnology, Government of India. K.G.H. thanks the Department of Biotechnology, Government of India, for the award of a postdoctoral fellowship. We thank S. Bala Tripura Sundari and K. Shanti for helpful discussions and Drs S. Harinarayana Rao, S. Rajanna and Satinder Rawat for help with the tissue collection.
PY - 1999/9/3
Y1 - 1999/9/3
N2 - We have studied the effect of guanosine-5'-O-(3-thiotriphosphate) (GTP-γ-S), a non-hydrolyzable analogue of GTP, on agonist and antagonist binding to bovine hippocampal 5-hydroxytryptamine (5-HT)(1A) receptor in native membranes. Our results show that the specific binding of the agonist is inhibited with increasing concentrations of GTP-γ-S along with a reduction in binding affinity. In sharp contrast to this, antagonist binding to 5-HT(1A) receptor shows no significant reduction and remains invariant over a large range of GTP-γ-S concentrations. The binding affinity of the antagonist also remains unaltered. This shows that the agonist and the antagonist differentially discriminate G-protein coupling of 5-HT(1A) receptors from bovine hippocampus. Copyright (C) 1999 Federation of European Biochemical Societies.
AB - We have studied the effect of guanosine-5'-O-(3-thiotriphosphate) (GTP-γ-S), a non-hydrolyzable analogue of GTP, on agonist and antagonist binding to bovine hippocampal 5-hydroxytryptamine (5-HT)(1A) receptor in native membranes. Our results show that the specific binding of the agonist is inhibited with increasing concentrations of GTP-γ-S along with a reduction in binding affinity. In sharp contrast to this, antagonist binding to 5-HT(1A) receptor shows no significant reduction and remains invariant over a large range of GTP-γ-S concentrations. The binding affinity of the antagonist also remains unaltered. This shows that the agonist and the antagonist differentially discriminate G-protein coupling of 5-HT(1A) receptors from bovine hippocampus. Copyright (C) 1999 Federation of European Biochemical Societies.
KW - 4-(2'-Methoxy)-phenyl-1-(2'-(N-2''-pyridinyl)-p-fluorobenzamido)ethyl-piperazine
KW - 5-Hydroxytryptamine(1A) receptor
KW - 8-Hydroxy-2-(di-N-propylamino)tetralin
KW - Bovine hippocampus
KW - G-protein coupling
KW - Guanosine-5'-O-(3-thiotriphosphate)
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U2 - 10.1016/S0014-5793(99)01082-0
DO - 10.1016/S0014-5793(99)01082-0
M3 - Article
C2 - 10471814
AN - SCOPUS:0032870924
SN - 0014-5793
VL - 457
SP - 389
EP - 392
JO - FEBS Letters
JF - FEBS Letters
IS - 3
ER -