TCS 46b

Names

[ Name ]:
TCS 46b

[Synonym ]:
tcs 46b

Biological Activity

[Description]:

TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[Target]

IC50: 5.3 nM (NR1A/2B), 35 μM (NR1A/2A), >100 μΜ (NR1A/2C), 0.5 μM (α-1 adrenergic receptor), 2.6 μM (dopamine D2)[1]

[In Vivo]

TCS 46b (Compound 46b; 10 and 30 mg/kg; p.o. or i.p.; once) 在 6-OHDA 损伤大鼠中增强左旋多巴的作用[1]。 Animal Model: Sprague−Dawley rats, 6-hydroxydopamine-lesioned (6-OHDA) rat model[1] Dosage: 10 and 30 mg/kg Administration: PO or IP, once Result: Showed significant potentiation of the effects of L-DOPA in this model.

[References]

[1]. Wright JL, et al. Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(heteroarylalkynyl)-4-benzylpiperidines. J Med Chem. 2000 Sep 7;43(18):3408-19.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₃N₃O

[ Molecular Weight ]:
345.44

[ Exact Mass ]:
345.18400

[ PSA ]:
51.89000

[ LogP ]:
3.10030

[ Storage condition ]:
-20°C

TCS 46b

Names

Biological Activity

Chemical & Physical Properties

Related Compounds