別包装 |
あり
|
分子量 |
342.82
|
CAS RN® |
34233-69-7
|
構造 |
C18H19ClN4O
|
使用目的 |
Clozapine N-oxide is a pharmacologically inert metabolite of Clozapine, which is a potent 5-HT1C receptor antagonist. Clozapine N-oxide (CNO) is a DREADD (designer receptors exclusively activated by designer drug) agonist.In Vivo:After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Acutely administered CNO can be metabolically converted to Clozapine in other species such as human and guinea-pig. The metabolites that may form after chronic administration of CNO to DREADD-expressing mice (or other species) have not been studied systematically. However, even if back-transformation to Clozapine occurs after chronic CNO administration, it should be noted that Clozapine is a more potent (by ~10-fold) DREADD agonist than CNO itself. Moreover, confounding biological effects of potential CNO metabolites can be easily identified by including both saline- and CNO-treated WT animals in a particular DREADD study. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h). One possibility is that CNO tends to accumulate in tissues, although other scenarios are also feasible[1]. Using a general pharmacokinetic model for the interconversion process, the mean total clearances of Clozapine and Clozapine N-oxide (CNO) are 28.45 L/hr and 45.30 L/hr, respectively[2].
|
参考文献 |
Biol Psychiatry. 2017 May 1;81(9):737-747.
|
[注意事項] |
[溶解度表記について]MCH社のWeb及びデータシート等で溶解度が「<1 mg/ml」のように記載されている場合、その化合物はその溶媒に、溶けないまたはわずかに溶けることを意味しています。(この場合、1mg/ml以下の濃度では試験していません。) 「>90mg/mL」のように記載されている場合、その化合物はその溶媒に90mg/ml で溶けたことを示しています。(ただし、最大でどのくらい溶けるかは試験していません。)
|
※サムネイル画像をクリックすると拡大画像が表示されます。
|
|
|
メーカー |
品番 |
包装 |
MCH
|
HY-17366
|
100 MG
|
※表示価格について
当社在庫 |
なし
|
納期目安 |
約10日
|
保存温度 |
-20℃
|
|