Characterization of a rat kidney thromboxane A2 receptor: high affinity for the agonist ligand I-BOP.
We have cloned a rat kidney thromboxane A2 receptor (TP) cDNA. This receptor was shown to be functional in that the thromboxane A2 mimetics, U46619 and I-BOP, elicited calcium transients in Xenopus oocytes and HEK293 cells expressing the TP receptor, respectively. Comparison of the affinities of the rat and human TP sites for the agonist radiolgand [125 I] BOP showed that the rat TP site has about a ten-fold higher affinity for this drug (KD approximately 0.5 vs. 4.4 nM) while the affinities of the two sites for other compounds (U46619, I-PTH-OH) were the same. Our results are significant in that they identify a cloned TP as having a picomolar affinity for [125 I] BOP.
D'Angelo
D D
DD
Division of Cardiology, University of Cincinnati, USA.
Terasawa
T
T
Carlisle
S J
SJ
Dorn
G W
GW
Lynch
K R
KR
D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism; D002478:Cells, Cultured; D003001:Cloning, Molecular; D004594:Electrophysiology; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology*; D006834:Hydrazines / Q000494:pharmacology; D007668:Kidney / Q000378:metabolism; D008297:Male; D008969:Molecular Sequence Data; D009865:Oocytes / Q000378:metabolism; D011450:Prostaglandin Endoperoxides, Synthetic / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D017482:Receptors, Thromboxane / Q000819:agonists / Q000737:chemistry*; D016415:Sequence Alignment; D017421:Sequence Analysis; D013928:Thromboxane A2 / Q000031:analogs & derivatives / Q000494:pharmacology; D014982:Xenopus laevis
D019086:Bridged Bicyclo Compounds, Heterocyclic; D005231:Fatty Acids, Unsaturated; D006834:Hydrazines; D011450:Prostaglandin Endoperoxides, Synthetic; D017482:Receptors, Thromboxane; C061750:7-(3-(3-hydroxy-4-(4'-iodophenoxy)-1-butenyl)-7-oxabicyclo(2.2.1)heptan-2-yl)-5-heptenoic acid; D013928:Thromboxane A2; D019796:15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid; C045749:SQ 29548; C046957:I-PTA-OH; D002118:Calcium