Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N,N-diethyl-N'-[(8a)-6-methylergolin-8-yl]-urea
Purity: ≥98%
Formula Markup: C20H28N4O
Formula Weight: 340.5
CAS Number: 37686-84-3
Notes: A receptor modulator; agonist of dopamine D2 and D3 receptors and the 5-HT receptor subtypes 5-HT1A, 5-HT1B, and 5-HT1D; induces 35SGTPγS binding in CHO cells expressing dopamine D2 or D3 receptors (EC50s = 0.46 and 0.66 nM, respectively, for the human receptors) or expressing 5-HT1A, 5-HT1B, and 5-HT1D (EC50s = 57.54, 426.58, and 14.13 nM, respectively, for the human receptors); antagonist of human α-adrenergic receptors (α-ARs; Kis = 3.55, 34.67, 3.89, 0.3, 0.45, and 0.76 nM for α1A-, α1B-, α1D-, α2A-, α2B-, and α2C-ARs, respectively), β1- and β2-ARs (Kis = 660.7 and 19.95 nM, respectively), the histamine H1 receptor (Ki = 338.84 nM), 5-HT2D, 5-HT2A, 5-HT2B, and 5-HT2C receptors (Kis = 16.22, 4.79, 7.08, and 47.86 nM, respectively), and dopamine D1-, D4-, and D5 receptors (Kis = 28.18, 8.13, and 7.63 nM respectively); inhibits 5-HT-induced vasoconstriction in rat isolated and perfused lungs at 1, 3, or 10 µM; inhibits monocrotaline-induced increases in pulmonary blood pressure, cardiac hypertrophy, and decreases in oxygen gas exchange in a rat model of pulmonary hypertension at 0.4 or 1.2 mg/kg per day
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