U-101958
U-101958 is a selective dopamine D4R antagonist. U-101958 binds to human D4 with a Ki of 1.4 nM and a pKi of 8.9. U-101958 inhibits Quinpirole (HY-B1752)-induced mitogenic effects. U-101958 can be used for research on schizophrenia.
For research use only. We do not sell to patients.
- CAS No.: 179556-82-2
- Formula: C21H29N3O
- Molecular Weight:339.47
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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
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Biological Activity
Description
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D4 Receptor 1.4 nM (Ki) |
In Vitro
U-101958 (20-50 μM) enhances presumed polysynaptic excitatory responses in Type II rat medial PFC pyramidal neurons[1].
U-101958 (1 μM; 1 h) binds the human dopamine D4 receptor with Ki 1.4 nM and has substantially lower affinity for dopamine D2 and the other tested receptors[2].
U-101958 (1 μM; 16-18 h) antagonizes Quinpirole (HY-B1752)-induced mitogenesis in CHO cells expressing the human dopamine D4 receptor[2].
U-101958 (concentration-response) antagonizes quinpirole-induced inhibition of K+-evoked [3H]GABA release in rat thalamic reticular nucleus slices with a Ki of 2.9 nM[3].
U-101958 (120 min) binds human recombinant D4.4 receptors in HEK293/D4 cell homogenates with pKi 8.9[4].
U-101958 (1×10-10-1×10-5 M; 15 min) is a full agonist at human recombinant D4.4 receptors in HEK293/D4 cells, inhibiting forskolin-stimulated cyclic AMP accumulation with pEC50 8.7 and 93% efficacy relative to dopamine[4].
U-101958 (1 μM; 120 min) binds human D4.4 receptors in CHO/D4 cell homogenates with pKi 8.9[6].
U-101958 (0.1 μM; 15 min) antagonizes dopamine-mediated cyclic AMP inhibition in CHO/D4 cells with pKB 8.9[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO cells expressing the human dopamine D4 receptor
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Concentration:1 μM
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Incubation Time:16-18 h (incubation); 2 h ([3H]thymidine)
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Result:Inhibited quinpirole-induced mitogenesis in CHO cells expressing the human dopamine D4 receptor at 1 μM, with the response plotted as a percentage of the quinpirole response.
Chemical Information
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CAS No. 179556-82-2
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Molecular Weight 339.47
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Formula C21H29N3O
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SMILES
CC(C)OC1=CC=CN=C1N(C2CCN(CC2)CC3=CC=CC=C3)C
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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]. Onn SP, et al. Dopamine D1 and D4 receptor subtypes differentially modulate recurrent excitatory synapses in prefrontal cortical pyramidal neurons. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2006 Feb;31(2):318-38. [Content Brief]
[4]. 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. British journal of pharmacology. 1998 Jul;124(5):889-96. [Content Brief]
[5]. Ma L, et al. Activation of glutathione peroxidase and inhibition of p53-related apoptosis by apomorphine. Journal of Alzheimer's disease : JAD. 2011;27(1):225-37. [Content Brief]
[6]. Gazi L, et al. Receptor density as a factor governing the efficacy of the dopamine D4 receptor ligands, L‐745,870 and U‐101958 at human recombinant D4. 4 receptors expressed in CHO cells. British journal of pharmacology. 1999 Oct;128(3):613-20. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
U-101958 Related Classifications
HY-189087 Related Classifications
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