U-101958 maleate
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.
For research use only. We do not sell to patients.
- CAS No.: 224170-09-6
- Formula: C25H33N3O5
- Molecular Weight:455.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Dopamine Receptor Isoforms
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Biological Activity
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D4 Receptor 2.7 nM (IC50) |
D3 Receptor 552 nM (IC50) |
D2 Receptor 1980 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
5500 nM
Compound: U-101958
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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.
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[PMID: 9873481] |
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.
Chemical Information
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CAS No. 224170-09-6
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Molecular Weight 455.55
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Formula C25H33N3O5
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SMILES
CC(C)OC1=CC=CN=C1N(C)C2CCN(CC2)CC3=CC=CC=C3.O=C(/C=C\C(O)=O)O
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Synonyms
PNU-101958 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
U-101958 maleate Related Classifications
HY-123663 Related Classifications
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