Platelet serotonin 5-HT2A receptor binding in patients with carcinoid tumor.
BACKGROUND
As carcinoid tumors produce and secrete serotonin, various serotonin markers in blood, plasma and urine have been used as diagnostic tools, and quantification of the urinary excretion of the serotonin metabolite 5-hydroxyindoleacetic acid (5-HIAA) is the method most frequently used.


METHODS
[3H]lysergic acid diethylamide ([3H]LSD) binding to the platelet serotonin 5-HT2A receptor was investigated in nine patients with carcinoid tumors. The possible effect of serotonin-rich food on the receptor binding was also investigated.


RESULTS
B(max) for [3H]LSD binding was significantly lower in the carcinoid group than in the control group (mean +/- SD: 17.6 +/- 1.3 vs. 23.9 +/- 5.2 fmol/mg protein; p = 0.007). Kd for [3H]LSD binding was significantly higher in the carcinoid group than in the control group (median: 1.14 vs. 0.71 nmol/L; p = 0.03). B(max) was inversely related to the urinary 5-HIAA excretion, but the correlation did not reach statistical significance (r(s) = -0.57; p = 0.14). Intake of five bananas per day for one week had no effect on B(max) or Kd in healthy volunteers.


CONCLUSIONS
The results are consistent with a down-regulation of the 5-HT2A receptor as a response to the high serotonin levels found in patients with carcinoid tumors. Intake of serotonin-rich food does not affect the receptor characteristics. Further studies are needed to determine whether the platelet 5-HT2A receptor status can be used as a supplement to urinary 5-HIAA and other biochemical variables in carcinoid tumors.
Spigset
O
O
Division of Clinical Pharmacology, University of Northern Sweden, Umeå, Sweden. olav.spigset@legemidler.no
Kristoffersson
A
A
Mjörndal
T
T
D000368:Aged; D014408:Biomarkers, Tumor / Q000652:urine; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D002276:Carcinoid Tumor / Q000175:diagnosis* / Q000378:metabolism; D015536:Down-Regulation; D005260:Female; D006801:Humans; D006897:Hydroxyindoleacetic Acid / Q000378:metabolism / Q000652:urine; D008238:Lysergic Acid Diethylamide / Q000378:metabolism / Q000494:pharmacology; D008297:Male; D008875:Middle Aged; D028521:Musa / Q000737:chemistry; D044402:Receptor, Serotonin, 5-HT2A / Q000097:blood / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism*
D014408:Biomarkers, Tumor; D044402:Receptor, Serotonin, 5-HT2A; D012701:Serotonin; D006897:Hydroxyindoleacetic Acid; D008238:Lysergic Acid Diethylamide