1-(2,3-二氢-1,4-苯并二恶烷-5-基)-4-[[5-(4-氟苯基)-3-吡啶基]甲基]哌嗪

生物活性靶点体外研究体内研究 1-(2,3-二氢-1,4-苯并二恶烷-5-基)-4-[[5-(4-氟苯基)-3-吡啶基]甲基]哌嗪试剂级价格

CAS号:222551-17-9
英文名:adoprazine
中文名:1-(2,3-二氢-1,4-苯并二恶烷-5-基)-4-[[5-(4-氟苯基)-3-吡啶基]甲基]哌嗪
CBNumber:CB51518488
分子式:C24H24FN3O2
分子量:405.46
MOL File:222551-17-9.mol

1-(2,3-二氢-1,4-苯并二恶烷-5-基)-4-[[5-(4-氟苯基)-3-吡啶基]甲基]哌嗪化学性质

沸点 :565.0±50.0 °C(Predicted)
密度 :1.256
储存条件 :Store at -20°C
溶解度 :DMSO : 50 mg/mL (123.32 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
形态 :Powder
酸度系数(pKa) :6.07±0.10(Predicted)
颜色 :Light yellow to yellow

1-(2,3-二氢-1,4-苯并二恶烷-5-基)-4-[[5-(4-氟苯基)-3-吡啶基]甲基]哌嗪性质、用途与生产工艺

生物活性 Adoprazine (SLV313) 是 5-HT 1A 受体的完全激动剂，其在 h5-HT1A 受体的 pEC50 为 9。Adoprazine (SLV313) 是 D2 和 D3 受体的完全拮抗剂，在 hD2 受体中的 pA2 值是 9.3，在 hD3 受体中的 pA2 值是 8.9。Adoprazine (SLV313) 具有非典型抗精神病的特征。

靶点

5-HT _1A Receptor

9 (pEC ₅₀ )

D ₂ Receptor

9.3 (pA2)

D ₃ Receptor

8.9 (pA2)

D ₄ Receptor

8.0 (pKi)

5-HT ₇ Receptor

7.2 (pKi)

5-HT _1A Receptor

9.1 (pKi)

D ₂ Receptor

8.4 (pKi)

D ₃ Receptor

8.4 (pKi)

体外研究

Adoprazine (SLV313) has high affinity at human recombinant D ₂ , D ₃ , D ₄ , 5-HT _2B , and 5-HT _1A receptors, with pK _i s of 8.4, 8.4, 8.0, 7.9 and 9.1, respectively. Adoprazine (SLV313) acts as a high potency dopamine D ₂ receptor antagonist and an efficacious serotonin 5-HT _1A receptor agonist, with E _max value (% effect of 10 μM 5-HT) of 73 and pK _B value of 8.5 .

体内研究

Adoprazine (SLV313) (0.1-10 mg/kg; p.o.; single) is sufficient to reduce extracellular 5-HT and increase dopamine levels in the nucleus accumbens in a dose- and time-dependent manner.

Animal Model:	Male Wistar rats (275-350 g)
Dosage:	0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration:	p.o.; single
Result:	Led to a dose- and time-dependent increase in extracellular levels of DA, DOPAC, and HVA. In contrast, led to a reduction in 5-HT levels and no change in 5-HIAA levels.