2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. 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].

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NGD 94-1 dimaleate

NGD 94-1 dimaleate Chemical Structure

CAS No. : 179333-18-7

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NGD 94-1 dimaleate Related Antibodies

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Description

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].

IC50 & Target[2]

hD4.2 Receptor

3.6 nM (Ki)

In Vitro

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.

NGD 94-1 dimaleate Related Antibodies
In Vivo

NGD 94-1 (1-5 mg/kg, i.m., 45 min prior to testing) (dimaleate) reverses the cognitive deficits and increases the accumulation of HVA in the cisternal cerebrospinal fluid of PCP pre-treated monkeys[1].

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

Animal Model: Young-adult vervet (Cercopithecus aethiops sabaeus) monkeys[1]
Dosage: 1 and 5 mg/kg
Administration: i.m., 45 min prior to testing
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.
Molecular Weight

552.54

Formula

C26H28N6O8
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NGD 94-1 dimaleate Related Classifications

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  • 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:

NGD 94-1 dimaleate179333-18-7Dopamine Receptordopamine D4 receptorhuman D4.2 receptorfrontostriatalPhencyclidinevervet monkeyInhibitorinhibitorinhibit

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