| CAS NO: | 945828-50-2 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 945828-50-2 |
| 化学名 | (E)-ethyl hydrogen (2-amino-4-((2,4,6-trimethylbenzyl)amino)phenyl)carbonimidate |
| Canonical SMILES | CCO/C(O)=N/C1=C(N)C=C(NCC2=C(C=C(C=C2C)C)C)C=C1 |
| 分子式 | C19H25N3O2 |
| 分子量 | 327.42 |
| 溶解度 | <32.74mg/ml in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | AA 29504, {2-amino-4-(2, 4, 6-trimethylbenzylamino)-phenyl}-carbamic acid ethyl ester is a positive modulator of extrasynaptic GABAA receptors. AA 29504 is also an analogue of the KCNQ channel opener retigabine with a 3-4 fold lower potency than retigabine. The EC50 of AA 29504 at KCNQ channels is between 9.6 and 13.5 μM [2]. AA 29504 at 1 μM had no agonist activity when tested at α1β3γ2s or α4β3δ GABAA receptors expressed in Xenopus oocytes, but left-shifted the EC50 of GABA and gaboxadol (THIP) at both receptors. The maximum GABA response was unchanged at α1β3γ2s receptors by AA 29504 (1 μM), but increased 3-fold at α4β3δ receptors [1]. GABA transiently activates synaptic GABAA receptors, leading to the classical inhibitory post-synaptic currents (phasic inhibition) [2]. KCNQ (also termed Kv7) channels are voltage-dependent potassium channels composed of homo- and heteromeric complexes of five different KCNQ subunits (KCNQ1–5, or called Kv7.1–Kv7.5) [3]. In Xenopus oocytes, AA 29504 at concentrations below 3 μM exhibited no intrinsic activity, whereas at 3 μM and above AA 29504 could induce a small response, which could not be blocked by bicuculline. Treatment with AA 29504 at a concentration of 1 μM showed no intrinsic activity at GABAA receptors and KCNQ channels, but left-shifted the concentration-response curve of GABA without affecting the maximum response to GABA [1]. In sub-chronic phencyclidine (PCP)-treated rats, acute administration of AA 29504 at 1 and 4 mg/kg reversed the PCP-induced deficit, but the middle dose of 2 mg/kg did not. Treatment with AA 29504 did not affect locomotor activity. AA 29504-treated animal groups were unable to significantly discriminate the novel objects from the familiar objects. The group treated with AA 29504 at 2 mg/kg showed a small but significant preference for the left object [2]. References: |
m.cnreagent.com