[125I]-PD151242: a selective radioligand for human ETA receptors - PubMed
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Br J Pharmacol
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. 1994 Jan;111(1):4-6.
doi: 10.1111/j.1476-5381.1994.tb14015.x.
[125I]-PD151242: a selective radioligand for human ETA receptors
A P Davenport 
1
, R E Kuc, F Fitzgerald, J J Maguire, K Berryman, A M Doherty
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1 Clinical Pharmacology Unit, University of Cambridge, Addenbrooke's Hospital.
PMID:
8012722
PMCID:
PMC1910024
DOI:
10.1111/j.1476-5381.1994.tb14015.x
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[125I]-PD151242: a selective radioligand for human ETA receptors
A P Davenport et al.
Br J Pharmacol.
1994 Jan.
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. 1994 Jan;111(1):4-6.
doi: 10.1111/j.1476-5381.1994.tb14015.x.
Authors
A P Davenport 
1
, R E Kuc, F Fitzgerald, J J Maguire, K Berryman, A M Doherty
Affiliation
1 Clinical Pharmacology Unit, University of Cambridge, Addenbrooke's Hospital.
PMID:
8012722
PMCID:
PMC1910024
DOI:
10.1111/j.1476-5381.1994.tb14015.x
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Our aim was to synthesize a new endothelin ETA selective radioligand, [125I]-PD151242 and characterize the compound in human vascular tissue. Binding of [125I]-PD151242 to sections of human aorta was time-dependent and reached equilibrium after 120 min at 23 degrees C with an association rate constant of 1.26 +/- 0.17 x 10(8) M-1 min-1 (n = 3 individuals +/- s.e.mean). The binding was reversible at 23 degrees C with an observed dissociation rate constant of 0.0025 +/- 0.0006 min-1 (n = 3). Saturation binding assays using [125I]-PD151242 revealed a single population of high affinity ET receptors (n = 3) in aorta (KD = 0.76 +/- 0.17 nM; Bmax = 5.98 +/- 1.56 fmol mg-1 protein), pulmonary (KD = 1.75 +/- 0.20 nM; Bmax = 12.78 +/- 1.39 fmol mg-1 protein) and coronary arteries (KD = 0.51 +/- 0.07 nM; Bmax = 44.9 +/- 1.67 fmol mg-1 protein). ETA selective ligands competed for [125I]-PD151242 binding in aorta with nanomolar affinity (BQ123, KD = 0.41 +/- 0.26 nM; FR139317, KD = 0.55 +/- 0.11 nM) whereas the ETB selective compound, BQ3020, competed with micromolar affinity (KD = 1.36 +/- 0.25 microM). In isolated coronary arteries, PD151242 was a functional antagonist and caused a significant, parallel rightward shift of the ET-1 dose-response curve with a pA2 value of 5.92 (n = 5) and a slope of unity. The high affinity and selectivity of [125I]-PD151242 for ETA receptors will facilitate the characterization of this sub-type in human tissues.
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References
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Life Sci. 1992;50(4):247-55
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J Med Chem. 1992 May 1;35(9):1493-508
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PubMed
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