302799-86-6

302799-86-6 structure

Name: TCS 46b
Chemical Name: 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzimidazol-2-one
CAS Number: 302799-86-6
Molecular Formula: C₂₂H₂₃N₃O
Molecular Weight: 345.44
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2017-06-04 15:14:36
Modify Date: 2026-07-01 12:53:28
TCS 46b (Compound 46b) is a potent, selective and orally active NMDA NR1A/2B receptor antagonist with an IC50 of 5.3 nM[1].

Name	5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzimidazol-2-one
Synonyms	1,3-Dihydro-5-[3-[4-(phenylmethyl)-H-benzimidazol-2-one 2H-Benzimidazol-2-one, 1,3-dihydro-5-[3-[4-(phenylmethyl)-1-piperidinyl]-1-propyn-1-yl] tcs 46b TCS 46B 5-(3-(4-Benzylpiperidin-1-yl)prop-1-yn-1-yl)-1,3-dihydro-2H-benzo[d]imidazol-2-one 5-(3-(4-benzylpiperidin-1-yl)prop-1-yn-1-yl)-1H-benzo[d]imidazol-2(3H)-one

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.