U-101958 maleate (Synonyms: PNU-101958 maleate)

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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.

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U-101958 maleate Estructura química

No. CAS : 224170-09-6

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

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Descripciòn

IC₅₀ & Target

D₄ Receptor

2.7 nM (IC₅₀)

D₃ Receptor

552 nM (IC₅₀)

D₂ Receptor

1980 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	5 nM Compound: U-101958	Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone	[PMID: 9873481]
CHO	IC₅₀	5500 nM Compound: U-101958	Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement. Binding affinity to cloned human Dopamine receptor D3 expressed in CHO cells by [3H]spiperone displacement.	[PMID: 9873481]
CHO	IC₅₀	8 nM Compound: U-101958	Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone	[PMID: 9873481]

In Vitro

U-101958 inhibits Forskolin (HY-15371)-stimulated cyclic AMP accumulation in HEK293/D4 cells in a concentration-dependent way^[1].
[3H]PNU-101958 is a D4 receptor probe. [3H]PNU-101958 binding sites in non-human primate brain appear to reflect D4 dopamine receptor distribution^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Peso molecular

455.55

Fòrmula

C₂₅H₃₃N₃O₅

No. CAS

224170-09-6

SMILES

CC(C)OC1=CC=CN=C1N(C)C2CCN(CC2)CC3=CC=CC=C3.O=C(/C=C\C(O)=O)O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

[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. [Content Brief]

U-101958 maleate Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

U-101958224170-09-6PNU-101958U101958U 101958PNU101958PNU 101958Dopamine ReceptorAntipsychoticInhibitorinhibitorinhibit

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