2. 疾病领域
  3. 神经系统疾病
  4. 神经退行性疾病
  5. 阿尔茨海默病
  6. AZD3676

AZD3676 是一种具有口服活性和血脑屏障通透性的 5-HT1ₐ 与 5-HT1ᵦ 受体配体，对人和猴的受体具有纳摩尔级结合亲和力 (human 5-HT1ₐ: 0.16 nM, monkey 5-HT1ₐ: 0.13 nM, human 5-HT1ᵦ: 2.3 nM, monkey 5-HT1ᵦ: 2.4 nM)。AZD3676 可用于阿尔茨海默病认知障碍的相关研究。

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AZD3676

AZD3676 Chemical Structure

CAS No. : 1259929-13-9

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AZD3676 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT1A and 5-HT1B receptors, with nanomolar binding affinity for human and monkey receptors (human 5-HT1A: 0.16 nM, monkey 5-HT1A: 0.13 nM, human 5-HT1B: 2.3 nM, monkey 5-HT1B: 2.4 nM). AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease[1].

体外研究
(In Vitro)

AZD3676 (1 pM-100 nM (5-HT1A); 0.01 nM-1 μM (5-HT1B); 16 h, room temperature) 在食蟹猴脑匀浆中对 5-HT1A (Ki = 0.13 nM) 和 5-HT1B (Ki = 2.4 nM) 受体表现出纳摩尔级亲和力[1]。
AZD3676 (0.4-20 μM; ~1 μM (predicted Cmax)) 呈现浓度依赖性的血浆蛋白结合特性，在预测的治疗最大浓度~1 μM 条件下，不同物种的游离分数范围为 0.014 (人) 至 0.37 (豚鼠)[1]。

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

AZD3676 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CLplasma Vdss AUC0-inf Cmax T1/2 Bioavailability
Rat[1] 1 mg/kg i.v. 83 mL/min/kg 5.2 L/kg / / / /
Rat[1] 1 mg/kg i.v. 83 mL/min/kg 5.2 L/kg / / / /
Rat[1] 3 mg/kg p.o. / / 0.3 μM·h 0.40 μM 0.7 h 21 %
Rat[1] 3 mg/kg p.o. / / 0.3 μM·h 0.40 μM 0.7 h 21 %
Dog[1] 1 mg/kg i.v. 37 mL/min/kg 3.5 L/kg / / / /
Dog[1] 1 mg/kg i.v. 37 mL/min/kg 3.5 L/kg / / / /
Dog[1] 3 mg/kg p.o. / / 1.3 μM·h 2.6 μM 2.8 h /
Dog[1] 3 mg/kg p.o. / / 1.3 μM·h 2.6 μM 2.8 h /
体内研究
(In Vivo)

AZD3676 (10 μmol/kg；皮下注射；单次给药) 可显著逆转 R-8-OH-DPAT 诱导的 C57BL/6 小鼠认知障碍，这一点可通过场景恐惧条件反射实验中恢复的僵住行为得到证实[1]。
AZD3676 (1-10 μmol/kg；皮下注射、口服；单次给药) 可显著逆转 Scopolamine (HY-N0296) 诱导的 C57BL/6 小鼠认知障碍，这一点可通过场景恐惧条件反射实验中恢复的僵住行为得到证明[1]。
AZD3676 (0.03-3 μmol/kg；皮下注射；单次给药) 可剂量依赖性地占据健康 C57BL/6 小鼠体内的 5-HT1ₐ受体，其前额叶皮层的半数最大受体占据剂量为 0.05 μmol/kg s.c.[1]。
AZD3676 (0.1-10 μmol/kg; 皮下注射; 单次给药) 可剂量依赖性地占据健康 Sprague Dawley 大鼠体内的 5-HT1A 受体，其前额叶皮层的半数最大受体占据剂量为 0.17 μmol/kg s.c.[1]。
AZD3676 (0.3-10 μmol/kg; s.c.; single dose) 在健康 Dunkin Hartley 豚鼠体内呈剂量依赖性地占据 5-HT1A 和 5-HT1B 受体，其半数最大受体占据值分别为 0.3 μmol/kg s.c. 和 1.2 μmol/kg s.c.[1]。
AZD3676 (0.16-0.82 μmol/kg；静脉注射；初始小剂量推注后维持输注) 可剂量依赖性地占据食蟹猴健康个体体内的 5-HT1A 受体，其前额叶皮层半数最大占据对应的血浆 Ki 值为 84 nM[1]。
AZD3676 (0.1-1.8 μmol/kg；静脉注射；初始小剂量推注后维持输注) 可剂量依赖性地占据食蟹猴健康个体体内的 5-HT1B 受体，其枕叶皮质半最大占据对应的血浆 Ki 为 72 nM[1]。

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

Animal Model: C57BL/6[1]
Dosage: 10 μmol/kg
Administration: s.c.; single dose
Result: Significantly reverted the R-8-OH-DPAT-induced memory deficit, as measured by increased freezing behavior relative to R-8-OH-DPAT-only treated mice.
Animal Model: C57BL/6[1]
Dosage: 3 μmol/kg; 10 μmol/kg; 1 μmol/kg
Administration: s.c.; single dose; p.o.; single dose
Result: Significantly reverted the scopolamine-induced memory deficit at 3 μmol/kg s.c., 10 μmol/kg s.c., and 1 μmol/kg p.o., as measured by increased freezing behavior relative to scopolamine-only treated mice.
Animal Model: C57BL/6[1]
Dosage: 0.03 μmol/kg; 0.1 μmol/kg; 0.3 μmol/kg; 1 μmol/kg; 3 μmol/kg
Administration: s.c.; single dose
Result: Dose-dependently occupied 5-HT1ₐ receptors in the mouse frontal cortex, with a half-maximum receptor occupancy of 0.05 μmol/kg s.c.
Animal Model: Sprague Dawley[1]
Dosage: 0.1 μmol/kg; 1 μmol/kg; 3 μmol/kg; 10 μmol/kg
Administration: s.c.; single dose
Result: Dose-dependently occupied 5-HT1ₐ receptors in the rat frontal cortex, with aa half-maximum receptor occupancy of 0.17 μmol/kg s.c.
分子量

378.48

Formula

C22H26N4O2
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

AZD3676 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

AZD36761259929-13-9AZD 3676AZD-3676rodent models5-HT1α receptor5-HT1β receptorC57BL/6 micecynomolgus monkey brain homogenatesDunkin Hartley guinea pigsAlzheimer’s diseaseSprague Dawley ratsnon-human primate braincynomolgus monkeysInhibitorinhibitorinhibit

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