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吩噻嗪 /Phenothiazine {[allProObj[0].p_purity_real_show]}

货号:A224816 同义名: Thiodiphenylamine;ENT 38

Phenothiazine, a dopamine2 (D2) receptor antagonist, could reduce the expression of dopamine in the brain.

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Phenothiazine 化学结构 CAS号:92-84-2
Phenothiazine 化学结构
CAS号:92-84-2
Phenothiazine 3D分子结构
CAS号:92-84-2
Phenothiazine 化学结构 CAS号:92-84-2
Phenothiazine 3D分子结构 CAS号:92-84-2
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Phenothiazine 纯度/质量文件 产品仅供科研

货号:A224816 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

+++

D4 receptor (human), Ki: 7.5 nM

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
Clozapine N-oxide 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Phenothiazine 生物活性

靶点
  • D2 receptor

描述 Phenothiazines are associated with elevated serum prolactin, which can suppress fertility in some species. Long-acting neuroleptic drugs reduce the adrenal stress response, but may interfere with reproductive responses and negatively influence breeding success[3]. Clinical use of N-substituted phenothiazines as antihistaminics (1940s), sedatives and antipsychotics (1950s) followed and continues to this day[4]. The synthesis of a series of novel phenothiazine compounds that inhibit the growth of both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. The more potent phenothiazine derivatives were more active against chloroquine-sensitive parasites than against chloroquine-resistant parasites and showed little synergy of action when used in combination with chloroquine[5].

Phenothiazine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00080444 Vomiting Phase 3 Completed - -
NCT00499746 - Completed - -
NCT00499746 Opioid Abuse ... 展开 >>Opioid Addiction Stimulant Abuse Stimulant Addiction 收起 << Phase 1 Phase 2 Completed - United States, Maryland ... 展开 >> Behavioral Pharmacology Research Unit Baltimore, Maryland, United States, 21224 收起 <<

Phenothiazine 参考文献

[1]Pluta K, Morak-Młodawska B, et al. Recent progress in biological activities of synthesized phenothiazines. Eur J Med Chem. 2011 Aug;46(8):3179-89.

[2]Hals PA, Hall H, et al. Phenothiazine drug metabolites: dopamine D2 receptor, alpha 1- and alpha 2-adrenoceptor binding. Eur J Pharmacol. 1986 Jun 24;125(3):373-81.

[3]Weiss RB, Schook MW, Wolfe BA. Long-acting neuroleptic use for reproductive management of non-domestic ungulates using the domestic goat (Capra hircus) as a model. Zoo Biol. 2014;33(3):204‐211

[4]Ohlow MJ, Moosmann B. Phenothiazine: the seven lives of pharmacology's first lead structure. Drug Discov Today. 2011;16(3-4):119‐131

[5]Kalkanidis M, Klonis N, Tilley L, Deady LW. Novel phenothiazine antimalarials: synthesis, antimalarial activity, and inhibition of the formation of beta-haematin. Biochem Pharmacol. 2002;63(5):833‐842

Phenothiazine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.02mL

1.00mL

0.50mL

25.09mL

5.02mL

2.51mL

50.18mL

10.04mL

5.02mL

Phenothiazine 技术信息

CAS号92-84-2
分子式C12H9NS
分子量 199.27
别名 Thiodiphenylamine;ENT 38;NSC-2037 NSC2037;NSC 2037
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 105 mg/mL(526.92 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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