caa a22 4500 465738907 CHVBK 20180323111803.0 cr unu---uuuuu 170327e19900301xx s 000 0 eng 10.1007/BF02244604 doi (NATIONALLICENCE)springer-10.1007/BF02244604 Effect on radiolabelled-monoamine uptake in vitro of plasma taken from healthy volunteers administered the antidepressant sibutramine HCl [Elektronische Daten] [Graham Luscombe, Nigel Slater, Michael Lyons, Ronan Wynne, Monte Scheinbaum, W. Roger Buckett] Sibutramine HCl, a monoamine reuptake inhibitor type of antidepressant, was administered to healthy male volunteers as either a single dose (12.5 or 50 mg) or repeated treatment (5-20 mg once daily or 15 mg twice daily). Plasma, obtained at regular intervals during and after sibutramine HCl or placebo treatment, was assayed in vitro for its ability to inhibit the uptake of [3H]-noradrenaline (NA) by rat cortical synaptosomes, [3H]-5-hydroxytryptamine (5HT) by human platelets and [14C]-dopamine (DA) by rat striatal synaptosomes. After both single and repeated sibutramine HCl administration, the rank order of uptake inhibition was [3H]-NA>[3H]-5HT>[14C]-DA. The level of monoamine uptake inhibition increased on daily administration to a plateau 4-6 days after initiation of treatment, for example, approximately 60% and 40% inhibition of [3H]-NA and [3H]-5HT, respectively, following 15 mg sibutramine HCl twice daily. The pattern of monoamine uptake inhibition following sibutramine HCl administration to man is similar to that observed in sibutramine HCl-treated rats, and probably at least partly reflects inhibition of uptake by drug metabolites in both species. The inhibition of monoamine uptake following sibutramine HCl administration to man is consistent with an antidepressant effect. Springer-Verlag, 1990 Sibutramine HCl nationallicence Antidepressant nationallicence Monoamine uptake inhibitor nationallicence Plasma nationallicence Human nationallicence Luscombe Graham Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut Slater Nigel Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut Lyons Michael Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut Wynne Ronan Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut Scheinbaum Monte The Boots Company (USA) Inc., 8800 Ellerbe Road, P.O. Box 6750, 71106-6750, Shreveport, LA, USA aut Roger Buckett W. Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut Psychopharmacology Springer-Verlag 100/3(1990-03-01), 345-349 0033-3158 100:3<345 1990 100 213 https://doi.org/10.1007/BF02244604 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF02244604 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Luscombe Graham Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut NATIONALLICENCE 700 1- Slater Nigel Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut NATIONALLICENCE 700 1- Lyons Michael Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut NATIONALLICENCE 700 1- Wynne Ronan Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut NATIONALLICENCE 700 1- Scheinbaum Monte The Boots Company (USA) Inc., 8800 Ellerbe Road, P.O. Box 6750, 71106-6750, Shreveport, LA, USA aut NATIONALLICENCE 700 1- Roger Buckett W. Boots Pharmaceuticals Research Department, NG2 3AA, Nottingham, UK aut NATIONALLICENCE 773 0- Psychopharmacology Springer-Verlag 100/3(1990-03-01), 345-349 0033-3158 100:3<345 1990 100 213 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer