Abstract
Changes in platelet serotonin uptake and content were investigated following administration of a single oral dose of 3-cyano-imipramine to healthy volunteers. The uptake of 3H-serotonin by platelets harvested from these subjects was almost completely inhibited 4 h after dose administration. This inhibition continued for at least 24 h. Plasma taken from the subjects inhibited the uptake of 3H-serotonin by platelets isolated from non-treated subjects. A small but significant reduction in platelet serotonin content was observed 3.75 h after dosing and was still evident after 24 h.
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Aberg-Wistedt A, Jostell K-G, Ross SB, Westerlund D (1981) Effect of zimelidine and desipramine on serotonin and noradrenaline uptake mechanisms in relation to plasma concentrations and to therapeutic effects during treatment of depression. Psychopharmacology 74: 297–305
Buus Lassen J, Squire RF, Christensen JA, Molander L (1975) Neurochemical and pharmacological studies on a new 5-HT uptake inhibitor, FG 4963 with potential antidepressant properties. Psychopharmacologia 42: 21–26
Buus Lassen J, Lund J, Bechgaard E, Sondergaard I (1979) Inhibition of 5-HT uptake into neurons and platelets in mice treated chronically with chlorimipramine and femoxetine. Psychopharmacology 64: 149–153
Drummond AH, Gordon JL (1974) Rapid sensitive microassay for platelet 5-HT. Thromb Diath Haemorrh 31: 366–367
Ehsanullah RSB (1980) Uptake of 5-hydroxytryptamine and dopamine into platelets from depressed patients and normal subjects —influence of clomipramine, desmethylclomipramine and maprotiline. Postgrad Med J 56 (suppl 1): 31–35
Gordon JL, Olverman HJ (1978) 5-Hydroxytryptamine and dopamine transport by rat and human blood platelets. Br J Pharmacol 62: 219–226
Haefely W, Schaffner R, Burkard W, Da Prada M, Keller HH, Pole P, Richards JG (1978) Ro 11-2465, a potent and selective inhibitor of 5-hydroxytryptamine uptake. 11th C.I.N.P. Congress Abstracts 95
Hyttal J (1977) Neurochemical characterization of a new potent and selective serotonin uptake inhibitor: Lu 10-171. Psychopharmacology 51: 225–233
Lemberger L, Rowe H, Carmichael R, Crabtree R, Horng JS, Bymaster F, Wong D (1978) Fluoxetine, a selective serotonin uptake inhibitor. Clin Pharmacol Ther 23: 421–429
Lenehan T, Omer LMO, Darragh A (1981a) Effect of Ro 11-2465, a new psychoactive agent on the uptake of serotonin by human platelets —in-vitro determination of the IC50. Arch Int Pharmacodyn Ther 249: 147–152
Lenehan T, Omer LMO, Kenny M, Lambe R, Darragh A (1981b) The effects of multiple rising doses of Ro 11-2465 (serotonin uptake inhibitor) on serotonin content of human platelets. Psychopharmacology 74: 1–3
Lindberg UH, Thorberg SO, Bengtsson S, Renyi AL, Ross SB, Ogren SO (1978) Inhibitors of neuronal monoamine uptake. 2. Selective inhibition of 5-hydroxytryptamine uptake by α-aminoacid esters of phenethyl alcohols. J Med Chem 21: 448–456
Lingjaerde O (1979) Inhibition of platelet uptake of serotonin in plasma from patients treated with clomipramine and amitriptyline. Eur J Clin Pharmacol 15: 335–340
Lund J, Lomholt B, Fabricius J, Christensen JA, Bechgaard E (1979) Paroxetine: Pharmacokinetics, tolerance and depletion of blood 5-HT in man. Acta Pharmacol Toxicol 44: 289–295
Pletscher A (1968) Metabolism, transfer and storage of 5-hydroxytryptamine in blood platelets. Br J Pharmacol Chemother 32: 1–6
Pletscher A (1978) Platelets as models for monoaminergic neurons. In: Youdim MBH (ed) Essays in neurochemistry and neuropharmacology, vol 3. Wiley, London, pp 49–101
Ross SB, Aperia B, Beck-Friis J, Jansa S, Wetterberg L, Aberg A (1980) Inhibition of 5-hydroxytryptamine uptake in human platelets by antidepressant agents in vivo. Psychopharmacology 67: 1–7
Sneddon JM (1973) Blood platelets as a model for monoaminecontaining neurones. In: Karkut CA, Phillis JW (eds) Progress in neurobiology. Pergamon, Oxford, pp 151–198
Stahl SM (1977) The human platelet. Arch Gen Psychiatry 34: 509–516
Stahl SM, Meltzer HY (1978) A kinetic and pharmacological analysis of 5-hydroxytryptamine transport by human platelets and platelet storage granules: Comparison with central serotonergic neurons. J Pharmacol Exp Ther 205: 118–132
Tuomisto J (1974) A new modification for studying 5-HT uptake by blood platelets: A re-evaluation of tricyclic antidepressants as uptake inhibitors. J Pharm Pharmacol 26: 92–100
Tuomisto J, Tukiainen E, Ahlfors UG (1979) Decreased uptake of 5-hydroxytryptamine in blood platelets from patients with endogenous depression. Psychopharmacology 65: 141–147
Wong DT, Bymaster FP, Horng JS, Molloy BB (1975) A new selective inhibitor for uptake of serotonin in synaptosomes of rat brain: 3-(p-trifluoromethylphenoxyl)-N-methyl-3-phenyl-propylamine. J Pharmacol Exp Ther 193:804–811
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Kenny, M., Lenehan, T.J., Lambe, R. et al. Effects of a single oral dose of 3-cyano-imipramine on serotonin uptake and content of platelets in healthy volunteers. Psychopharmacology 79, 304–307 (1983). https://doi.org/10.1007/BF00433406
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DOI: https://doi.org/10.1007/BF00433406