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Calcitriol is a hormone and the active form of vitamin D, normally made in the kidney. [ 8 ] [ 9 ] [ 10 ] It is also known as 1,25-dihydroxycholecalciferol . It binds to and activates the vitamin D receptor in the nucleus of the cell, which then increases the expression of many genes. [ 11 ]
The natural, active form of vitamin D is calcitriol (1,25-dihydroxycholecalciferol). This molecule and other naturally occurring forms of vitamin D, including its precursors and metabolites, have been modified to synthesize pharmaceuticals with potentially greater, or selective, therapeutic actions.
The vitamin D receptor (VDR also known as the calcitriol receptor) is a member of the nuclear receptor family of transcription factors. [5] Calcitriol (the active form of vitamin D , 1,25-(OH) 2 vitamin D 3 ) binds to VDR, which then forms a heterodimer with the retinoid-X receptor .
Calcitriol plays a key role in regulating vitamin D levels through a negative feedback mechanism. [203] It strongly upregulates the expression of the enzyme CYP24A1 , which inactivates vitamin D. This activation happens through binding of the activated vitamin D receptor (VDR) to two vitamin D response elements (VDREs) in the CYP24A1 gene.
Eldecalcitol is an analog of calcitriol, the active form of vitamin D. [1]Commonly used in Japan for the treatment of osteoporosis. [2] Osteoporosis is a common bone disease among the older generation, with an estimated prevalence of over 200 million people. [2]
Calcitroic acid (1α-hydroxy-23-carboxy-24,25,26,27-tetranorvitamin D 3) is a major metabolite of 1α,25-dihydroxyvitamin D 3 (calcitriol). [1] Around 1980, scientists first reported the isolation of calcitroic acid from the aqueous extract of radioactively treated animals' livers and intestines.
Calcipotriol, also known as calcipotriene, is a synthetic derivative of calcitriol, a form of vitamin D. It is used in the treatment of psoriasis. [1] It is safe for long-term application in psoriatic skin conditions. [medical citation needed] It was patented in 1985 and approved for medical use in 1991. [2]
Paricalcitol (chemically it is 19-nor-1,25-(OH) 2-vitamin D 2.Marketed by Abbott Laboratories under the trade name Zemplar) is a drug used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic kidney failure.
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