NGD94-1
Based on 1 Customer Validation
NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research[1][2].
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- Pureté: 99.79%
- CAS No.: 178928-68-2
- Formule: C18H20N6
- Masse moléculaire:320.39
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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hD4.2 Receptor 3.6 nM (Ki) |
NGD 94-1 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 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. 178928-68-2
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Appearance Solid
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Masse moléculaire 320.39
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Formule C18H20N6
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Color White to off-white
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SMILES
C1(N2CCN(CC3=CN=C(C4=CC=CC=C4)N3)CC2)=NC=CC=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Pureté et documentation
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Fiche technique (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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)
NGD94-1 Related Classifications
HY-103405 Related Classifications
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