1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. TPMPA

TPMPA 是异四氢烟酸和 3-APMPA 的混合物,是 GABAC 的第一个选择性拮抗剂 (KB = 2.1 μM),但不与 GABAA (KB = 320 μM) 或 GABAB (EC50 = 500 μM) 受体相互作用。TPMPA 具有抑制神经节细胞定向选择性的潜力。

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TPMPA Chemical Structure

TPMPA Chemical Structure

CAS No. : 182485-36-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells[1][2][3].

IC50 & Target

KB: 2.1 μM (GABAC)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Oocyte IC50
2.22 μM
Compound: 3, TPMPA
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
22.09 μM
Compound: 3, TPMPA
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte EC50
500 μM
Compound: 3, TPMPA
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte EC50
500 μM
Compound: 3, TPMPA
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
[PMID: 18528996]
体外研究
(In Vitro)

TPMPA antagonizes the GABA currents of ρ1 receptors (IC50 = 1.6 μM) and those of the chimeric ρ1/α1 receptors with approximately the same potency (IC50 = 1.3 μM)[1].
TPMPA shows weak activity against rho-1 and rho-2 receptors, with the KB values of 2.0 and 15.6 μM, respectively[2]

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

分子量

161.14

Formula

C6H12NO2P

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

纯度 & 产品资料
参考文献
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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:
TPMPA
目录号:
HY-101359
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