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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Dopamine Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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D4 Receptor 2.7 nM (IC50) |
D3 Receptor 552 nM (IC50) |
D2 Receptor 1980 nM (IC50) |
Cellular Effect
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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] |
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. Further protocols information, click here.
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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