2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. BP1.3656B

BP1.3656B 是一种选择性的、口服有效的、可通过血脑屏障的组胺 H3 受体 (histamine H3 receptor) 反向激动剂/拮抗剂，其拮抗激动剂诱导活性的 KB 为 0.08 nM，直接抑制受体基础活性的 IC50 为 0.38 nM。BP1.3656B 可减少饮酒行为、寻酒行为、酒精自服行为、饮酒动机、酒精复吸、酒精诱导的运动亢进以及酗酒摄入。BP1.3656B 可用于酒精使用障碍的研究。

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BP1.3656B

BP1.3656B Chemical Structure

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BP1.3656B 相关抗体

Top Publications Citing Use of Products

查看 Histamine Receptor 亚型特异性产品:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BP1.3656B is a selective, orally active, blood-brain barrier-permeable histamine H3 receptor (histamine H3 receptor) inverse agonist/antagonist, with a KB value of 0.08 nM for antagonizing agonist-induced activity and an IC50 value of 0.38 nM for directly inhibiting the basal activity of the receptor. BP1.3656B reduces alcohol consumption, alcohol-seeking behavior, alcohol self-administration, motivation to drink, alcohol relapse, alcohol-induced hyperlocomotion, and binge alcohol intake. BP1.3656B is applicable for the research of alcohol use disorder[1].

IC50 & Target[1]

H3 receptor

0.38 nM (IC50)

体内研究
(In Vivo)

BP1.3656B (0.003-1 mg/kg；口服；单次给药) 可剂量依赖性地升高雄性 OF1 小鼠脑内 t-MeHA 水平，其 ED50 为 0.008 mg/kg[1]。
BP1.3656B (0.03-0.1 mg/kg; 腹腔注射；单次给药) 可剂量依赖性地升高雄性 Wistar 大鼠海马区的细胞外乙酰胆碱水平[1]。
BP1.3656B (0.005-0.3 mg/kg；单次给药) 可降低雌性 DBA/2J 小鼠中酒精诱导的运动过度活跃[1]。
BP1.3656B (0.3 mg/kg；腹腔注射；每日给药；连续 4 天) 可使雌性 DBA/2J 小鼠中酒精诱导的运动致敏性在连续 4 天的治疗中降低 31%-44%[1]。
BP1.3656B (0.3 mg/kg；腹腔注射；单次给药) 可使雄性小鼠在黑暗饮酒模型中的酗酒摄入量降低 25%；使酒精戒断期间小鼠的类焦虑行为恢复正常；使非成瘾和酒精依赖性雄性大鼠的酒精自主摄取量降低[1]。

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

Animal Model: DBA/2J (female)[1]
Dosage: 0.005 mg/kg; 0.03 mg/kg; 0.3 mg/kg
Administration: i.p.; single dose
Result: Reduced alcohol-induced locomotor activity by 37%.
Reduced alcohol-induced locomotor activity by 39%.
Animal Model: DBA/2J (female)[1]
Dosage: 0.3 mg/kg
Administration: i.p.; daily; 4 consecutive days
Result: Reduced alcohol-induced locomotor sensitization by 31% on day 1, 44% on day 2, 25% on day 3, and 40% on day 4.
Animal Model: C57BL/6J (male)[1]
Dosage: 0.3 mg/kg
Administration: i.p.; singe dose
Result: Reduced 2-hour binge alcohol intake by 25%.
Increased time spent in the open arms of the elevated plus maze
Animal Model: Long Evans (male; non-dependent)[1]
Dosage: 0.3 mg/kg
Administration: i.p.; single dose
Result: Reduced active lever presses by 70%, alcohol consumption by 73%, and motivation (breakpoint) by 43% compared to placebo.
Reduced alcohol relapse by 44% on the first day post-extinction, with effects maintained across relapse sessions.
Animal Model: Long Evans (male; alcohol-dependent)[1]
Dosage: 0.3 mg/kg
Administration: i.p.; single dose
Result: Reduced active lever presses by 46%, alcohol consumption by 55%, and motivation (breakpoint) by 44% compared to placebo.
Completely blocked alcohol relapse on the first day post-extinction, with effects maintained across relapse sessions.
分子量

399.35

Formula

C20H28Cl2N2O2
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

BP1.3656B 相关分类

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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:

BP1.3656BHistamine ReceptorhippocampusHEK-293 cellsfemale DBA/2J micehistamine H3 receptoralcohol use disordermale C57BL/6J micemale OF1 micemale Wistar ratsacetylcholinemale Long Evans ratsInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-181960
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