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MRK-016

CAS No. : 342652-67-9

MCE 站：MRK-016

产品活性：MRK-016 是一种选择性的，可口服的，可透过血脑屏障的 GABA_A α5 receptor 拮抗剂，对 GABA_A α5 的 EC₅₀ 值为 3 nM，对人 GABA_A?α1β3γ2，GABA_A?α2β3γ2，GABA_A?α3β3γ2 和 GABA_A?α5β3γ2 的 K_i 值分别为 0.83，0.85，0.77?和 1.4?nM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GABA Receptor

In Vitro: MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77?and 1.4?nM for human?GABA_A?α1β3γ2, GABA_A?α2β3γ2, GABA_A?α3β3γ2, and GABA_A?α5β3γ2, respectively. MRK-016 is a full inverse agonist at the α5-subtype, shows very weak affinity at the GABA_A α4β3γ2-subtype (K_i 395 ± 173 nM) and is essentially inactive at the GABA_A α6β3γ2 receptor (K_i > 4000 nM). MRK-016 shows a weak effect on GABA_A?α4β3γ2 with a K_i of 400 nM. MRK-016 (100 nM) alao increases long-term potentiation in mouse hippocampal slices.

In Vivo: MRK-016 does not enhance pentylenetetrazole-induced convulsions at 10 mg/kg via ip, or cause seizures at 30 mg/kg, via po for 20 days in mice. MRK-016 shows no obvious anxiogenic-like effects in rats at doses that occupy >95% of benzodiazepine (BZ) binding sites. MRK-016 (0.3, 1, and 3 mg/kg, p.o.) dose-dependently improves performance of rats hippocampal-dependent memory task. MRK-016 (0.3-30 mg/kg, p.o.) causes good receptor occupancy in rats. MRK-016 (0.3, 1, or 3 mg/kg p.o.) shows cognition-enhancing activity in the delayed matching-to-position version of the Morris water maze. MRK-016 (1, 3, or 10 mg/kg i.p.) does not produce kindling in mice. MRK-016 (3 mg/kg, i.p.) protects against LPS-induced learning/memory decrements in mice.

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