Abstract
Ro 11-2465, a cyanide derivative of imipramine with serotonin uptake inhibitory properties, was investigated in six healthy volunteers for its effect on serotonin concentration in blood platelets. The initial dose was 1 mg daily, the maximum dose of 3 mg being reached on day 3 and maintained for 7 days.
A significant decrease in the platelet serotonin concentration was not observed until 3 days after the start of drug administration, after which depletion was rapid. After 5 days of treatment, the reduction was about 80% compared to predrug level. Serotonin restoration after drug withdrawal was very slow, and 5 days after discontinuation, it was still 70% below its baseline level.
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References
Drummond AH, Gordon JL (1974) Rapid sensitive microassay for platelet 5-HT. Thromb Diath Haemorrh 31:366–367
Garattini J, Valzelli L (1965) Serotonin. Elsevier, Amsterdam London New York, pp 57–71
Haefely W, Schaffner R, Burkard W, Da Prada M, Keller HH, Polc P, Richards JG (1978) Ro 11-2465, a potent and selective inhibitor of 5-hydroxytryptamine uptake. 11th C.I.N.P. Congress Abstract 95
Marshall EF, Stirling GS, Tait AC, Todrick A (1960) The effect of iproniazid and imipramine on the blood platelet 5-hydroxytryptamine level in man. Br J Pharmacol 15:35–41
Ross SB, Jansa S, Wetterberg I, Fyrö B, Hellner B (1976) Decreased blood level of 5-hydroxytryptamine by inhibitors of the membranal 5-hydroxytryptamine uptake. Life Sci 19:205–210
Todrick A, Tait AC (1969) The inhibition of human platelet 5-hydroxytryptamine uptake by tricyclic antidepressive drugs. The relation between structure and potency. J Pharm Pharmacol 21:751–762
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Lenehan, T., Omer, L.M.O., Kenny, M. et al. The effect of multiple rising doses of Ro 11-2465 (serotonin uptake inhibitor) on serotonin content of human platelets. Psychopharmacology 74, 1–3 (1981). https://doi.org/10.1007/BF00431746
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DOI: https://doi.org/10.1007/BF00431746