1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR Calcium Channel
  3. PAM-2

PAM-2 是一种强效、口服有效、可穿透血脑屏障的选择性 α7 nAChR 正向变构调节剂 (human α7 nAChR EC50:39 μM,rat α7 nAChR EC50:12 μM),具有抗痛觉过敏和抗炎活性。PAM-2 对 α9α10 nAChR (IC50 = 174 μM) 和 CaV2.2 通道 (IC50 = 89 μM) 表现出选择性。PAM-2 通过增强 α7 nAChR 活性,减轻 Streptozotocin (STZ) (HY-13753) 和 Oxaliplatin (HY-17371) 诱导的小鼠神经病理性疼痛。PAM-2 可用于神经病理性疼痛的研究。

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PAM-2

PAM-2 Chemical Structure

CAS No. : 1426293-61-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain[1].

IC50 & Target[1]

human α7 nAChR

39 μM (EC50)

rat α7 nAChR

12 μM (EC50)

CaV2.2

89 μM (IC50)

α9α10 nAChR

174 μM (IC50)

体外研究
(In Vitro)

PAM-2 (0.3 μM-1 mM;5 分钟) 以浓度依赖的方式增强 Xenopus 卵母细胞中乙酰胆碱 (30 μM) 激活的 α7 nAChRs 活性[1]
PAM-2 (0.3 μM-1 mM;2 分钟) 以浓度依赖性且电压无关的方式抑制非洲爪蟾卵母细胞中 rα9α10 nAChRs 对乙酰胆碱 (10 μM) 诱发的电流[1]
PAM-2 (0.3 μM-1 mM) 在 HEK293 细胞中抑制 Cav2.2 通道介导的 Ba2+电流,而不影响 G 蛋白偶联的 GABABR[1]

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

体内研究
(In Vivo)

PAM-2 (1 和 3 mg/kg;口服;在 STZ 后第 15 天单次给药) 可减轻小鼠的 STZ 和 Oxaliplatin 诱导的神经病理性疼痛[1]
PAM-2 (1 mg/kg;口服;与 Oxaliplatin 联合给药 14 天;在最后一次联合给药后 30 分钟额外给药一次) PAM-2 与 Oxaliplatin 共同给药 14 天可预防疼痛,追加给药可提高痛阈[1]

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

Animal Model: Male CD-1 albino mice (2-3 months old) intraperitonealy injected with STZ (100 mg/kg)[1]
Dosage: 1, 3 mg/kg
Administration: p.o.; single dose on day 15 post-STZ
Result: Significantly decreased neuropathic pain between 15 and 45 min at 3 mg/kg, 45 min, with complete reversal at 30 min.
Showed no effect at 1 mg/kg.
Animal Model: Male CD-1 albino mice (2-3 months old) intraperitonealy injected with Oxaliplatin (2.4 mg/kg) on days 1-3, 6-10, and 13-14[1]
Dosage: 1, 3 mg/kg
Administration: p.o.; single dose on day 15 post-Oxaliplatin
Result: Significantly decreased neuropathic pain from 15 to 45 minutes after administration, with peak reversal at 30 min at 3 mg/kg.
Showed no effect at 1 mg/kg.
Animal Model: Male CD-1 albino mice (2-3 months old) intraperitonealy injected with Oxaliplatin (2.4 mg/kg) on days 1-3, 6-10, and 13-14[1]
Dosage: 1 mg/kg
Administration: p.o; coadministered with oxaliplatin schedule for 14 days; and an extra dose 30 min post last co-treatment
Result: Prevented pain establishment by day 14.
An additional administration on the test day produced greater pain reversal within 0-30 min.
分子量

227.26

Formula

C14H13NO2

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
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  • 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.

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产品名称:
PAM-2
目录号:
HY-180400
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