Disease relevance of Deacetylmoxisylyte

• In pentobarbitone-anaesthetized normotensive rats, prazosin, thymoxamine and deacetylthymoxamine decreased the hypotensive effect of clonidine, but had no significant effect on clonidine-induced bradycardia [1].
• Clonidine-induced reduction of tachycardia caused by electrical stimulation of the cardiac sympathetic nerve in pithed rats was antagonized by phentolamine but not by prazosin, thymoxamine, deacetylthymoxamine or N-demetyldeacetylthymoxamine [1].

High impact information on Deacetylmoxisylyte

• The two sulphate derivatives (deacetylmoxisylyte sulphoconjugate, DAM-S and monomethyldeacetylmoxisylyte sulphoconjugate, MDAM-S), were analysed without prior hydrolysis [2].
• Thymoxamine was found to permeate the cornea and to be hydrolysed very quickly, showing very good absorption with a maximum aqueous humor concentration of deacetylthymoxamine of 2329 ng/ml 15 min after eye drop instillation [3].
• At the level of the thoracic aorta, the three drugs act as antagonists with a dual mode of action (thymoxamine pA2 = 6.55--pD2' = 4.70; deacetylthymoxamine pA2 = 6.53--pD2' = 4.70; N-demethyldeacetylthymoxamine pA2 = 5.61--pD2' = 4.63) [4].

Analytical, diagnostic and therapeutic context of Deacetylmoxisylyte

• The metabolite was identified as desacetylthymoxamine by HPLC, spectrophotometry and direct inlet mass spectrometry [5].

References