1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. NGD94-1

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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NGD94-1

NGD94-1 화학구조

CAS No. : 178928-68-2

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제품 설명

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].

IC50 & Target[2]

hD4.2 Receptor

3.6 nM (Ki)

In Vitro

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.

In Vivo

NGD94-1 (1-5 mg/kg, i.m., 45 min prior to testing) 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.
분자량

320.39

화학식

C18H20N6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(N2CCN(CC3=CN=C(C4=CC=CC=C4)N3)CC2)=NC=CC=N1

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

순도&문서
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상품명:
NGD94-1
Cat. No.:
HY-103405
수량:
MCE Japan Authorized Agent: