Desglymidodrine (Synonyms: ST 1059) |
| カタログ番号GC52051 |
ミドドリンの活性代謝物であるデスグリミドリン (ST 1059) は、選択的 α1 アドレナリン受容体アゴニストです。
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Cas No.: 3600-87-1
Sample solution is provided at 25 µL, 10mM.
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Desglymidodrine is the active metabolite of the prodrug midodrine .1 It is formed from midodrine by enzymatic hydrolysis.2 Desglymidodrine is an agonist of α1-adrenergic receptors (α1-ARs).1 It binds to α1-ARs (Kis = 9.77, 9.55, and 8.51 µM for α1A, α1B, and α1D-ARs, respectively) and increases intraurethral pressure (IUP) and mean arterial pressure (MAP) by 5 and 20 mm Hg, respectively, in anesthetized dogs at doses of 205 and 250 nmol/kg, respectively.
1.Altenbach, R.J., Khilevich, A., Kolasa, T., et al.Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing α1A-adrenoceptor agonistJ. Med. Chem.47(12)3220-3235(2004) 2.McClellan, K.J., Wiseman, L.R., and Wilde, M.I.Midodrine. A review of its therapeutic use in the management of orthostatic hypotensionDrugs Aging12(1)76-86(1998)
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