| Identification | Back Directory | [Name]
2-Pyridinamine, N-methyl-3-(1-methylethoxy)-N-[1-(phenylmethyl)-4-piperidinyl]-, (2Z)-2-butenedioate (1:1) | [CAS]
224170-09-6 | [Synonyms]
2-Pyridinamine, N-methyl-3-(1-methylethoxy)-N-[1-(phenylmethyl)-4-piperidinyl]-, (2Z)-2-butenedioate (1:1) | [Molecular Formula]
C25H33N3O5 | [MOL File]
224170-09-6.mol | [Molecular Weight]
455.56 |
| Hazard Information | Back Directory | [Description]
U-101958 Maleate is a dopamine D4 receptor ligand. U-101958 Maleate also binds to a large sigma1 receptor-like component in human cerebellum and SK-N-MC neuroblastoma cells with high affinity. | [Uses]
U-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC50 of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic[1][2]. | [IC 50]
D4 Receptor: 2.7 nM (IC50); D3 Receptor: 552 nM (IC50); D2 Receptor: 1980 nM (IC50) | [References]
[1] Gazi L, et al. The agonist activities of the putative antipsychotic agents, L-745,870 and U-101958 in HEK293 cells expressing the human dopamine D4.4 receptor. Br J Pharmacol. 1998 Jul;124(5):889-96. DOI:10.1038/sj.bjp.0701921
[2] De La Garza R 2nd, et al. [(3)H]PNU-101958, a D(4) dopamine receptor probe, accumulates in prefrontal cortex and hippocampus of non-human primate brain. Synapse. 2000 Sep 1;37(3):232-44. DOI:10.1002/1098-2396(20000901)37:3<232::AID-SYN7>3.0.CO;2-7 |
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| Company Name: |
Merck KGaA
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21-20338288 |
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www.sigmaaldrich.cn |
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