Research Tazarotene.docVIP

 PAGE \* MERGEFORMAT 16 Research Tazarotene [Abstract] Tazarotene is the first receptor-selective, third generation aromatase-dimensional A acid drugs, mainly selective combination of two kinds of dimension A acid receptor (RAR-β; RAR-γ), but not with the Victoria A acid X receptor (RXR) binding. Clinical safe and effective for the treatment of psoriasis, acne, and for abnormal keratinization disorders, hair follicles, sebaceous gland diseases, skin cancer, precancerous lesion, clinical development and application of a bright future.  A name, chemical structure, structure-activity relationship and metabolism of [1,2] Tazarotene (tazarotene) or acetylene-dimensional A acid (acetylenic retinoid), trade name acetylene-dimensional (China Chongqing Winbond), molecular formula C21H21NO2S. Tazarotene linear-shaped molecules to replace the original single-double bond triple bond polyene chain to form a rigid structure, dual-aryl acetylene can only apply to certain dimensional acid A receptor, because there is no isomer, does not A different dimension of potential lead acid receptor activity, the drug molecule in the structural design of the original part of free carboxylic acid ester prodrug with the B instead of the form, which in the local effects and toxicity of the model showed that a better therapeutic index. Structure, the introduction of nicotinic acid, in order to ensure the rapid metabolism of tazarotene acetate married aqueous free acid (tazarotene acid) form, thus avoiding savings and addicted to drugs in the body fatty acids Victoria A long half-life drug problems. The sulfur atoms into addicted fat ring, in order to facilitate the appropriate molecules are rapidly metabolized cytochrome isoenzymes oxidized sulfur, or sulfoxide, and sulfone. This oxidation pathway of drug metabolism in the body quickly, activity disappears.  2 mechanism [3,4] Tazarotene 2.1 receptor selective nuclear receptor modulators by activating g