title: Evidence for dopaminergic binding sites in the human adrenal cortex.
abstract: Dopamine may be a modulator of aldosterone secretion in man. Whether this effect is extraadrenal or is exerted directly at the adrenal gland via local dopaminergic receptors remains uncertain. This study examined the possibility that dopaminergic binding sites exist in the human adrenal cortex using [3H]spiperone, a butyrophenone with high affinity for dopaminergic receptors of the D2 subtype. [3H]Spiperone binding to membranes prepared from the outer adrenal cortex obtained from eight patients undergoing adrenalectomy was studied. Specific [3H]spiperone binding, defined as binding displacable by 250-fold excess of unlabeled spiperone reached equilibrium within 30 minutes at 4 degrees C and was readily reversible. Binding was consistent with both high affinity (Kd1 = 0.2 to 0.8 nmol/L) and low affinity (Kd2 = 20 to 127 nmol/L) binding states. Binding capacity was 27 to 276 fmol/mg for the high affinity and 63 to 597 fmol/mg for the low affinity binding state. The relative potency in inhibition of [3H]spiperone binding was as follows: antagonists, spiperone greater than domperidone greater than metoclopramide greater than ketanserin greater than (-) sulpiride greater than (+) sulpiride; agonists, dopamine, bromocriptine greater than NPA much much greater than epinephrine. Serotonin and norepinephrine did not affect [3H]spiperone binding. These data suggest the existence of dopaminergic binding sites possibly of the D2 subtype in the human adrenal cortex. The precise location of these sites remains to be determined.
mesh_terms: D000302:Adrenal Cortex / Q000032:analysis*; D000328:Adult; D000368:Aged; D001058:Apomorphine / Q000031:analogs & derivatives / Q000378:metabolism; D001667:Binding, Competitive; D001971:Bromocriptine / Q000378:metabolism; D004294:Domperidone / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D004837:Epinephrine / Q000378:metabolism; D005260:Female; D006801:Humans; D007650:Ketanserin / Q000378:metabolism; D008297:Male; D008787:Metoclopramide / Q000378:metabolism; D008875:Middle Aged; D011954:Receptors, Dopamine / Q000032:analysis*; D013134:Spiperone / Q000378:metabolism; D013469:Sulpiride / Q000378:metabolism; D013997:Time Factors
chemical_list: D011954:Receptors, Dopamine; D001971:Bromocriptine; D013134:Spiperone; D004294:Domperidone; C009074:N-n-propylnorapomorphine; D013469:Sulpiride; D007650:Ketanserin; D008787:Metoclopramide; D001058:Apomorphine; D004298:Dopamine; D004837:Epinephrine