2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. RTICBM-74

RTICBM-74 是一种可穿透血脑屏障的、选择性的 CB1 变构调节剂，其 IC50 值为 23 nM (钙动员测定) 和 153 nM ([35S]GTPγS 测试)。RTICBM-74 可抑制 CB1 受体信号传导。RTICBM-74 可减少大鼠的酒精摄入量。RTICBM-74 可用于酒精使用障碍的研究。

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RTICBM-74

RTICBM-74 Chemical Structure

CAS No. : 2130881-32-0

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RTICBM-74 相关抗体

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CB1 CB2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder[1].

IC50 & Target[1]

CB1

23 nM (IC50)

CB1

153 nM (IC50)

体外研究
(In Vitro)

RTICBM-74 (1 μM; 15-240 min) 在雄性 Sprague-Dawley 大鼠肝细胞中表现出优异的代谢稳定性，半衰期为 461 分钟，固有清除率为 14.5 mL/min/kg[1]。
RTICBM-74 (1 μM; 6 h) 与大鼠血浆蛋白高度结合，在平衡条件下该化合物的结合率达 99.9%[1]。
RTICBM-74 在大鼠肝微粒体中表现出优异的代谢稳定性，半衰期超过 300 分钟，固有清除率低于 4.6 mL/min/kg[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RTICBM-74 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax (Plasma) CL/F AUCinf Cmax (Brain) Tmax (Brain)
Rat[1] 10 mg/kg i.p. 70.2 (Plasma) ng/mL 6.0 (Plasma) h 119.4 (Plasma) mL/min/kg 1476.2 (Plasma) ng·h/mL 272.0 ng/mL 4.5 (Brain) h
体内研究
(In Vivo)

RTICBM-74 (5-10 mg/kg；腹腔注射；单次) 可特异性减少雌性 Long-Evans 大鼠的酒精自主摄取量[1]。
RTICBM-74 (腹腔注射；单次，剂量 7.5-10 mg/kg) 可特异性减少雄性 Wistar 大鼠的酒精自主摄取行为，且不会引发运动障碍[1]。
RTICBM-74 (腹腔注射；单次，剂量 7.5-10 mg/kg) 对雄性 Wistar 大鼠的蔗糖自主摄取或自发活动无影响，证实其减少酒精摄入作用的特异性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Long-Evans (female, adult, alcohol self-administration trained via sucrose fading on fixed ratio 2 schedule for ~4 months)[1]
Dosage: 5 mg/kg; 7.5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced alcohol lever responses (F(3, 30) = 7.90; P < 0.0001).
Reduced alcohol intake from vehicle 0.53 g/kg to 0.40 g/kg (5 mg/kg), 0.42 g/kg (7.5 mg/kg), and 0.17 g/kg (10 mg/kg) (F(3,30) = 9.18; P<0.001).
Reduced alcohol lever responses in the first 5 minutes of the session at 7.5 and 10 mg/kg doses.
Reduced alcohol lever responses from the second 5-minute bin onward at all three doses.
Reduced locomotor rate and sucrose lever responses from vehicle 7.90 mL/kg to 5.38 mL/kg (10 mg/kg) (F(3,30) = 5.52; P<0.01).
Animal Model: Wistar (male, adult, alcohol self-administration trained via sucrose fading on fixed ratio 2 schedule for ~4 months)[1]
Dosage: 7.5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced alcohol lever responses (F(2, 20) = 4.79; P < 0.05).
Reduced alcohol intake from vehicle 0.65 g/kg to 0.43 g/kg (7.5 mg/kg) and 0.44 g/kg (10 mg/kg) (F(2,20) = 4.07; P<0.01).
Reduced alcohol lever responses at the 15-minute time bin at 7.5 mg/kg dose.
Reduced alcohol lever responses at the 20, 25, and 30-minute time bins at 10 mg/kg dose.
Caused no changes to locomotor rate or inactive lever presses.
Animal Model: Wistar (male, adult, sucrose self-administration trained on fixed ratio 2 schedule)[1]
Dosage: 7.5 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Caused no significant effects on sucrose lever responses.
Caused no significant effects on sucrose intake (vehicle: 12.28 mL/kg; 7.5 mg/kg: 10.88 mL/kg; 10 mg/kg: 8.37 mL/kg; F(2,20) = 1.96; P<0.05).
Caused no changes to locomotor rate or inactive lever presses.
分子量

340.78

Formula

C19H14ClFN2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

RTICBM-74 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RTICBM-742130881-32-0RTICBM74RTICBM 74Cannabinoid Receptorratsion channelsSprague-Dawley rat hepatocytesGPCRsLong-Evans ratsMDCK-mdr1 cellsCB1 receptoralcohol use disordertransportersrat liver microsomesInhibitorinhibitorinhibit

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