I'm very interested in this compound, it's been described as "the best cup of green tea you've ever had". I have yet to sample it for myself, but want to get some soon. It's a thiamine derivative and "its initial transport rate is 20-times faster than for thiamine." (PMID: 8186267, listed below)
Here are some abstracts:
: Pharmacol Biochem Behav. 1985 Aug;23(2):195-8. Related Articles, Links
Chronic administration of sulbutiamine improves long term memory formation in mice: possible cholinergic mediation.
Micheau J, Durkin TP, Destrade C, Rolland Y, Jaffard R.
Thiamine deficiency in both man and animals is known to produce memory dysfunction and cognitive disorders which have been related to an impairment of cholinergic activity. The present experiment was aimed at testing whether, inversely, chronic administration of large doses of sulbutiamine would have a facilitative effect on memory and would induce changes in central cholinergic activity. Accordingly mice received 300 mg/kg of sulbutiamine daily for 10 days. They were then submitted to an appetitive operant level press conditioning test. When compared to control subjects, sulbutiamine treated mice learned the task at the same rate in a single session but showed greatly improved performance when tested 24 hr after partial acquisition of the same task. Parallel neurochemical investigations showed that the treatment induced a slight (+ 10%) but significant increase in hippocampal sodium-dependent high affinity choline uptake. The present findings and previous results suggest that sulbutiamine improves memory formation and that this behavioral effect could be mediated by an increase in hippocampal cholinergic activity.
PMID: 4059305 [PubMed - indexed for MEDLINE]
1: Rev Electroencephalogr Neurophysiol Clin. 1982 Dec;12(4):373-8. Related Articles, Links
[Facilitation of a state of wakefulness by semi-chronic treatment with sulbutiamin (Arcalion) in Macaca mulatta]
[Article in French]
Balzamo E, Vuillon-Cacciuttolo G.
Cortical electroencephalographic (EEG) activities and nycthemeral states of vigilance organization were studied in 6 adult rhesus monkeys during subchronic administration (10 days) of Sulbutiamin, a synthesized derivative of thiamine (300 mg/kg/day). Sulbutiamin induced the following modifications: (1) In the EEG activities: increase in occurrence of fast rhythms (over 28 c/sec) during waking and also during slow sleep (SS) in which their amplitude doubled. SS spindles increased in number and amplitude. (2) In vigilance organization: waking was enhanced all along the 24 h recording and SS was reorganized (particularly at night), mostly light sleep: large decrease in stage 2 duration, increase in stage 1. REM sleep duration remained stable. These changes, occurring at around day 5 of the treatment, were more pronounced on day 10 and disappeared 2-5 days after withdrawal. This study demonstrated the clear action of Sulbutiamin upon the mechanisms regulating waking and light sleep.
PMID: 7170385 [PubMed - indexed for MEDLINE]
1: Biochim Biophys Acta. 1994 May 26;1222(1):7-14. Related Articles, Links
The compartmentation of phosphorylated thiamine derivatives in cultured neuroblastoma cells.
Bettendorff L.
Laboratory of General and Comparative Biochemistry, University of Liege, Belgium.
Thiamine transport in cultured neuroblastoma cells is mediated by a high-affinity carrier (KM = 40 nM). In contrast, the uptake of the more hydrophobic sulbutiamine (isobutyrylthiamine disulfide) is unsaturable and its initial transport rate is 20-times faster than for thiamine. In the cytoplasm, sulbutiamine is rapidly hydrolyzed and reduced to free thiamine, the overall process resulting in a rapid and concentrative thiamine accumulation. Incorporation of radioactivity from [14C]thiamine or [14C]sulbutiamine into intracellular thiamine diphosphate is slow in both cases. Despite the fact that the diphosphate is probably the direct precursor for both thiamine monophosphate and triphosphate, the specific radioactivity increased much faster for the latter two compounds than for thiamine diphosphate. This suggests the existence of two pools of thiamine diphosphate, the larger one having a very slow turnover (about 17 h); a much smaller, rapidly turning over pool would be the precursor of thiamine mono- and triphosphate. The turnover time for thiamine triphosphate could be estimated to be 1-2 h. When preloading the cells with [14C]sulbutiamine was followed by a chase with the same concentration of the unlabeled compound, the specific radioactivities of thiamine and thiamine monophosphate decreased exponentially as expected, but labeling of the diphosphate continued to increase slowly. Specific radioactivity of thiamine triphosphate increased first, but after 30 min it began to slowly decrease. These results show for the first time the existence of distinct thiamine diphosphate pools in the same homogeneous cell population. They also suggest a complex compartmentation of thiamine metabolism.
PMID: 8186267 [PubMed - indexed for MEDLINE]
1: Encephale. 2000 Mar-Apr;26(2):70-5. Related Articles, Links
[Effects of sulbutiamine (Arcalion 200) on psycho-behavioral inhibition in major depressive episodes]
[Article in French]
Loo H, Poirier MF, Ollat H, Elatki S.
Service Hospitalo-Universitaire de Sante Mentale et de Therapeutique, Hopital Sainte-Anne, Paris.
Psycho-behavioural inhibition is characteristic of major depressive disorder and frequently recedes after the other depressive symptoms. This may induce an important psychosocial impairment which could be a risk factor for relapse. METHODS: The aim of this eight weeks, multicentric, randomized, double blind, placebo controlled trial was to assess the efficacy and safety of sulbutiamine (Arcalion) [600 mg p.d.] on the symptoms of psycho-behavioural inhibition of inpatients with DSM III-R defined Major Depressive Episode (MDE) treated by adjusted doses of clomipramine [75 to 150 mg pd]. Moderate doses of hypnotics and anxiolytics without potential activity on the mood were authorized during the trial. The MDE was assessed with the MADRS, HAM-A and CGI scales. Patients who did not respond adequately to the antidepressant treatment were prematurely withdrawn from the trial. The three Sheehan Disability Scales (SDS), the Norris Visual Analogue Scale (VAS) and the Depressive Psychomotor Retardation Scale (ERD) were used to monitor psycho-behavioural inhibition. RESULTS: The mean intake scores were, as expected, fairly high: MADRS (32), HAMA-A (23), CGI (5) and ERD (27). The SDS and EVA scores showed that the patients felt severely handicapped in their social, professional and family life functioning as well as in their emotional, affective, cognitive and behavioural performances. At four weeks the MADRS, HAM-A and CGI scores indicated that the global improvement of the MDE was comparable in both treatment groups. However, the scores at the EVA and SDS scales showed that the patients treated with sulbutiamine were significantly less incapacitated than the placebo group in all of the various facets (affective, cognitive, emotional, behavioural) of psycho-behavioural inhibition. Furthermore, the safety data shows that both treatment groups were comparable and in particular that sulbutiamine had not induced any inappropriate behaviour, including suicide attempts, or mania. CONCLUSIONS: Sulbutiamine has no antidepressive effect but it can hasten the resorption of psycho-behavioural inhibition occurring during major depressive disorder and thereby facilitate the rehabilitation of patients in their social, professional and family life functioning.
Publication Types:
* Clinical Trial
* Multicenter Study
* Randomized Controlled Trial
PMID: 10858919 [PubMed - indexed for MEDLINE]
