Platelet alpha 2-adrenoceptors, defined with agonist and antagonist ligands, in depressed patients, prior to and following treatment.
Saturation binding of the alpha 2-adrenoceptor antagonist, 3H-yohimbine, and displacement of 3H-yohimbine with the alpha 2-adrenoceptor agonist, UK-14,304, were performed concurrently in platelet membranes obtained from drug-free depressed patients and healthy volunteers. Where possible platelet binding was repeated in depressed patients following treatment. The number and affinity of 3H-yohimbine binding sites did not differ between controls and depressed patients, or when depressed patients were divided on the basis of endogenicity (Newcastle or RDC criteria) or dexamethasone test result. The proportion of alpha 2-adrenoceptor binding sites with high affinity for UK-14,304 and KD values for the two states of the receptor did not differ in the total sample of depressed patients compared to controls. The KD for both states of the receptor and the proportion of sites with high affinity for UK-14,304 was lower in RDC non-endogenous patients than RDC endogenous patients. Treatment did not alter the total number of alpha 2-adrenoceptors or the proportion of sites with high affinity for UK-14,304, but reduced the KD for 3H-yohimbine and the KD of UK-14,304 for the low affinity state of the alpha 2-adrenoceptor.
Department of Pharmacology and Clinical Pharmacology, St George's Hospital Medical School, London, U.K.
A E
AE
Theodorou
K M
KM
Lawrence
D
D
Healy
A M
AM
Whitehouse
W
W
White
H
H
Wilton-Cox
S M
SM
Kerry
R W
RW
Horton
E S
ES
Paykel
D000316:Adrenergic alpha-Agonists / Q000493:pharmacokinetics*; D001667:Binding, Competitive / Q000187:drug effects; D001792:Blood Platelets / Q000187:drug effects* / Q000378:metabolism*; D000068438:Brimonidine Tartrate; D003866:Depressive Disorder / Q000097:blood* / Q000628:therapy*; D004565:Electroconvulsive Therapy; D006801:Humans; D007099:Imipramine / Q000627:therapeutic use*; D008127:Lofepramine / Q000627:therapeutic use*; D011569:Psychiatric Status Rating Scales; D011810:Quinoxalines / Q000493:pharmacokinetics*; D011869:Radioligand Assay; D011941:Receptors, Adrenergic / Q000187:drug effects* / Q000378:metabolism*; D015016:Yohimbine / Q000493:pharmacokinetics*
D000316:Adrenergic alpha-Agonists; D011810:Quinoxalines; D011941:Receptors, Adrenergic; D015016:Yohimbine; D000068438:Brimonidine Tartrate; D008127:Lofepramine; D007099:Imipramine