CAS NO: | 5588-33-0 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 386.57 |
Cas No. | 5588-33-0 |
Formula | C21H26N2OS2 |
Solubility | insoluble in H2O; ≥16.35 mg/mL in DMSO; ≥3.1 mg/mL in EtOH |
Chemical Name | 10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylsulfinyl)-10H-phenothiazine |
Canonical SMILES | CN1CCCCC1CCN2C3=C(C=CC(S(C)=O)=C3)SC4=C2C=CC=C4 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Mesoridazine is a dopaminergic antagonist, with aKdvalue of 19 nM for the dopamine D2 receptor. Mesoridazine is an active metabolite of the atypical antipsychotic drug thioridazine, exhibiting stronger inhibition on pre- and postsynaptic dopamine receptors which modulate dopamine and acetylcholine release. Thus, mesoridazine is responsible for a significant part of the antidopaminergic effects attributed to thioridazine. In addition, mesoridazine also binds to histamine H1, muscarinic acetylcholine, as well as α1- and α2-adrenergic receptors, withKdvalues being 1.8, 69, 2 and 1600 nM, respectively.
References:
1. Niedzwiecki DM, Cubeddu LX, Mailman RB. Comparative antidopaminergic properties of thioridazine, mesoridazine and sulforidazine on the corpus striatum. Journal of Pharmacology and Experimental Therapeutics, 1989, 250(1): 117-125.
2. Richelson E, Nelson A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brainin vitro. European Journal of Pharmacology, 1984, 103(3-4): 197-204.
3. Shah NS. Influence of psychotropic drugs and β-diethylaminoethyl-diphenylpropylacetate (SKF 525-A) on mescaline-induced behavior and on tissue levels of mescaline in mice. Biochemical Pharmacology, 1976, 25(5): 591-597.
Animal experiment:[3] | |
Animal models | Swiss-Webster albino mice, 30~33 g |
Dosage form | 10, 30 and 45 mg/kg Intraperitoneal Injection |
Applications | Mesoridazine (10 mg/kg) did not completely abolish the locomotor activity, but did prevent the activity-increasing effect of mescaline. At high doses of 30 and 45 mg/kg, mesoridazine blocked not only the activity-increasing effect of mescaline but also the normal locomotor movements. |
Note | The technical data provided above is for reference only. |
References: 1. Niedzwiecki DM, Cubeddu LX, Mailman RB. Comparative antidopaminergic properties of thioridazine, mesoridazine and sulforidazine on the corpus striatum. Journal of Pharmacology and Experimental Therapeutics, 1989, 250(1): 117-125. 2. Richelson E, Nelson A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. European Journal of Pharmacology, 1984, 103(3-4): 197-204. 3. Shah NS. Influence of psychotropic drugs and β-diethylaminoethyl-diphenylpropylacetate (SKF 525-A) on mescaline-induced behavior and on tissue levels of mescaline in mice. Biochemical Pharmacology, 1976, 25(5): 591-597. |