Phenothiazine

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Chemical Structure| 92-84-2 同义名 : Thiodiphenylamine; ENT 38; NSC-2037 NSC2037; NSC 2037
CAS号 : 92-84-2
货号 : A224816
分子式 : C12H9NS
纯度 : 98%
分子量 : 199.27
MDL号 : MFCD00005015
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
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
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].
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 <<
实验方案
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
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