High affinity radioligands

Hawkey CJ (1999) COX-2 inhibitors. Lancet 353 307-314 Hedberg A, Hall SE, Ogletree ML et al. (1988) Characterization of [5,6-3H]SQ 29,548 as a high affinity radioligand, binding to thromboxane A2/prostaglandin H2-receptors in human platelets. J Pharmacol Exp Ther 245 786-792... 

IJI.AB-MECA, 3, was introduced as a high affinity radioligand for A3 receptors [21]. 

Chen Y, Falck JR, Tuniki VR, Campbell WB (2009) 20- Iodo-14,15-epoxyeicosa-5(Z)-enoic acid a high-affinity radioligand used to characterize the epoxyeicosatrienoic acid antagonist binding site. J Pharmacol Exp Ther 331 1137-1145... 

An iodinated radioligand that speeilically labels the agonist high affinity state of 5-HT2 serotonin receptors. J Med Chem 31 5-7, 1988. 

Since oocytes are a transient, small-scale expression system, they are not the best suited for radioligand binding studies as (usually) hundreds of oocytes must be injected to harvest sufficient membranes for such measurements. This is both time-consuming and expensive. However, with high affinity and highly specific activity ligands, the expression of binding sites on the membranes of intact oocytes can be readily quantified (see later). 

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