NGD 94-1 dimaleate
NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research[1][2].
For research use only. We do not sell to patients.
- CAS No.: 179333-18-7
- Formula: C26H28N6O8
- Molecular Weight:552.54
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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
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hD4.2 Receptor 3.6 nM (Ki) |
NGD 94-1 (dimaleate) shows >600-fold selectivity for the D4.2 receptor over many other targets; however, its selectivity is significantly lower over the 5-HT1A (~50-fold) and 5-HT3 (~200-fold) receptors[2].
NGD 94-1 (dimaleate) induces inhibition of cAMP accumulation in HEK293/D4 cells, but does not affect Forskolin (HY-15371)-stimulated cAMP formation in non-transfected HEK293 cells, demonstrating that its inhibitory action is specifically mediated through the transfected dopamine D4 receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Young-adult vervet (Cercopithecus aethiops sabaeus) monkeys[1]
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Dosage:1 and 5 mg/kg
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Administration:i.m., 45 min prior to testing
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Result:Significantly reversed the impaired successful performance of PCP-treated subjects (from 58% to 79% accuracy) at 1 mg/kg.
Ameliorated the PCP-induced impairments (from 73% to 86% accuracy) at 5 mg/kg.
Reduced barrier reaching and perseverative responding at both doses in PCP-treated monkeys.
Unaffected response initiation latencies and motor problems in PCP-treated monkeys.
Unaffected accurate performance at 1 mg/kg in saline pretreated monkeys.
Slightly impaired successful performance at 5 mg/kg in saline pretreated monkeys.
Failed to affect response initiation latencies or motor problems at both doses in saline pretreated monkeys.
Failed to affect HVA levels relative to saline in control subjects.
Significantly increased HVA concentrations in the CSF in PCP-treated subjects.
Chemical Information
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CAS No. 179333-18-7
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Molecular Weight 552.54
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Formula C26H28N6O8
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SMILES
O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.C1(N2CCN(CC3=CN=C(C4=CC=CC=C4)N3)CC2)=NC=CC=N1
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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]. Jentsch JD, et al. Dopamine D4 receptor antagonist reversal of subchronic phencyclidine-induced object retrieval/detour deficits in monkeys. Psychopharmacology (Berl). 1999 Feb;142(1):78-84. [Content Brief]
[2]. Tallman JF, et al. I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor. J Pharmacol Exp Ther. 1997 Aug;282(2):1011-9. [Content Brief]
[3]. Gazi L, et al. NGD 94-1 as an agonist at human recombinant dopamine D4.4 receptors expressed in HEK293 cells. Eur J Pharmacol. 1999 May 21;372(3):R9-10. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NGD 94-1 dimaleate Related Classifications
HY-103405A Related Classifications
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