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. 1992 May;106(1):101–108. doi: 10.1111/j.1476-5381.1992.tb14300.x

Imidazoline binding sites in human placenta: evidence for heterogeneity and a search for physiological function.

S Diamant 1, T Eldar-Geva 1, D Atlas 1
PMCID: PMC1907438  PMID: 1324063

Abstract

1. An alpha 2-adrenoceptor antagonist, idazoxan, that binds to both alpha 2-adrenoceptors and to imidazoline sites (IR), has been used to characterize human placental IR. Human placenta is shown to be the richest source of IR (1800 +/- 100 fmol mg-1 protein; Kd 38.9 +/- 3.4 nM). 2. Primary cells derived from human placenta and grown in monolayers, also displayed a high density of receptors (3209 +/- 136 fmol mg-1 in cytotrophoblasts and 3642 +/- 144 fmol mg-1 protein in syncytiotrophoblast enriched cell culture). 3. [3H]-idazoxan did not show binding characteristics of alpha 2-adrenoceptors in human placental membranes or human trophoblastic cells, thus making it a ligand of choice to study the imidazoline site. The tissue appeared to be lacking alpha 2-adrenoceptors in that other alpha 2-adrenoceptor ligands, [3H]-rauwolscine and [3H]-clonidine, do not bind to alpha 2-adrenoceptors in human placenta. 4. IRs are localized on the cell surface, as determined by the release of bound [3H]-idazoxan from cells, when washed with high ionic/acidic medium. 5. Imidazoline receptors of human placenta display high affinity for amiloride (72 +/- 27 nM). The high affinity was used as a criterion to classify IR to IRa subtype (placenta, rabbit kidney, rabbit liver and rabbit adipose cells) as opposed to the IRb subtype which display low affinity for amiloride (greater than 2 microM, in all the other tissues).(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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