Disease relevance of Dexamisole

• A series of tetramisole derivatives was synthesized and tested for inhibitory activity against alkaline phosphatase which was partially purified from a murine ascitic neoplasm resistant to 6-thiopurines (Sarcoma 180/TG) [1].
• Levamisole, the 1-isomer of tetramisole, is rapidly and completely absorbed, but has not been widely used in systemic helminthiases because of severe side effects associated with prolonged dosage [2].
• The results suggest nervous involvement in the acute toxicity of tetramisole [3].
• Transient optic neuritis following tetramisole [4].
• Comparison of pyrantel and tetramisole in ascariasis [5].

Psychiatry related information on Dexamisole

• Both doses of tetramisole significantly increased stereotyped behavior of the mice on days 3, 5 and 8 in comparison with respective control values [3].
• Daily treatment of mice with tetramisole at 0.5 and 1mg/kg for six consecutive days did not significantly affect their general locomotor activity in the open-field activity test [3].

High impact information on Dexamisole

• This phenotype was suppressed by inhibiting muscle contraction by a myosin mutation, but it was enhanced by tetramisole-induced hypercontraction [6].
• Effect of L- and D-tetramisole on 32Pi and 45Ca uptake and mineralization by matrix vesicle-enriched fractions from chicken epiphyseal cartilage [7].
• Reaction of 3-amino derivatives of the nematocides tetramisole and levamisole with variously substituted benzoylisocyanates gave a series of benzoylureas I which were tested for activity against helminths and ectoparasites [8].
• Tetramisole and its analogues are potent inhibitors of alkaline phosphatase, including isoenzymes of Sarcoma 180/TG which appear to be involved in the mechanism of resistance of this neoplastic cell line to the 6-thiopurines [9].
• The findings support the concept that the thiazole ring system of the tetramisole structure is required for maximum inhibitory potency of this series against alkaline phosphatase [9].

Chemical compound and disease context of Dexamisole

• To determine the requirement for the thiazole ring system of tetramisole for inhibitor potency, 2,3,5,6-tetrahydro-6-phenylimidazo[2,1-b]oxazole, 2,3-dihydro-6-phenylimidazo[2,1-b]oxazole, and 2,3,5,6-phenylimidazo[2,1-a]imidazole were synthesized and tested for inhibitory activity against alkaline phosphatase isolated from Sarcoma 180/TG [9].
• Antagonization of tetramisole toxicity by hexamethonium [10].
• In 1 group, 5 sheep, which were treated twice with tetramisole at an interval of 4 weeks to remove gastro-intestinal nematodes and lungworms, showed an increase of 41% in weight gain and 3.2% in wool growth compared with an untreated group [11].
• Another group, which was treated with both tetramisole and rafoxanide to remove nematode and fluke infections, had a 143% increase in weight gain and 81% in wool growth compared with the control [11].
• The strategic use of single therapeutic doses of closantel, tetramisole or sustained low-level administration of albendazole in feed pellets in controlling naturally acquired parasitic gastroenteritis in sheep was investigated on a farm in semi-arid Rajasthan, India. A total of 303 5- to 6-month-old sheep were divided into three groups [12].

Biological context of Dexamisole

• A commercially available pharmaceutical, tetramisole, was found to be a competent enantioselective acylation catalyst [13].
• Although tetramisole showed no effect on cell growth and increased hydroxyproline accumulation, it decreased the osteocalcin production and the accumulation of calcium and phosphate in the matrices [14].
• The most successful treatment occurred in SPF (Specific Pathogen Free) rats dosed with tetramisole loaded into zeolite and no worms were present in this group at autopsy eight days post-infection [15].

Anatomical context of Dexamisole

• When live worms were implanted and tetramisole was not given, lesions developed in 3 of 6 testes [16].
• Determination of the partition of the tetramisole derivative (+-)-5,6-dihydro-6-phenyl-2-n-propyl-imidazo[2,1-b]thiazole into liposomal membranes by fluorescence quenching of the membrane probe 8-(2-anthryl)-octanoic acid [17].
• Contraction of cat nictitating membrane by tetramisole [18].
• The major structural changes observed after treatment with all the drugs were vacuolation in the intestine of H. contortus except with TP treatment and disruption of the epithelium in T. globulosa except with TMS treatment [19].

Associations of Dexamisole with other chemical compounds

• This activity appears to be from an acid phosphatase because it was enhanced at low pH values, was inhibited by the acid phosphatase inhibitor sodium fluoride, and was not inhibited by the alkaline phosphatase inhibitor tetramisole [20].
• Fluorescence quenching has been used to study the partition of the tetramisole derivative (+-)-5,6-dihydro-6-phenyl-2-n-propyl-imidazo[2,1-b]thiazole into liposomes, consisting of a mixture of egg L-alpha-phosphatidylcholine, egg phosphatidylethanolamine and dipalmitoylphosphatidic acid (2:1:0.06 w/w/w) [17].
• Interactions of tetramisole, imidazo[2,1-b]thiazolic derived or immunomodulatory agents with human serum albumin (HSA) and immunoglobulins G and A has been investigated in vitro using polyacrylamide gel electrophoresis and immunoelectrophoresis [21].
• Nippostrongylus brasiliensis was found to be sensitive to thiabendazole, tetramisole and levamisole but the broad spectrum anthelmintic mebendazole was ineffective [22].

Gene context of Dexamisole

• Acute toxicity and neurobehavioral effects of the veterinary anthelmintic tetramisole were examined in male albino mice [3].
• The ecto-5'-nucleotidase activity was insensitive to levamisole and tetramisole, inhibitors of alkaline phosphatases, whereas alpha,beta-methylene-ADP inhibited the enzymatic activity of both strains [23].
• Treatment of Nippostrongylus brasiliensis in normal and SPF rats using tetramisole loaded into zeolite [15].

Analytical, diagnostic and therapeutic context of Dexamisole

• High-pressure liquid chromatography was used with a 10-micron C8-type bonded silica gel column to quantitate the tetramisole in veterinary anthelmintic preparations [24].
• The effects of levamisole (LT), dexamisole (DT), levo-p-bromotetramisole (LBT) and dextro-p-bromotetramisole (DBT) on bone were examined in an organ culture system using calvarial bones from newborn mice [25].
• Subcutaneous injection of tetramisole at 0.5 and 1mg/kg did not significantly affect general locomotor activity of the mice in 5-min open-field activity test or negative geotaxis performance and landing foot splay [3].
• However, the 1mg/kg dose of tetramisole significantly increased the stereotyped behavior (grooming, sniffing, biting and licking and head bobbing) of the mice when compared to the control group [3].
• On the other hand, in the group treated with tetramisole, the mean faecal egg count rose from 3 weeks after treatment and remained continuously higher than those in any other group up to 12 weeks after treatment [12].

References