NGD94-1

Cat. No.: HY-103405: Ficha de datos
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NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (K_i = 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 Estructura química

No. CAS : 178928-68-2

Tamaño	Precio	Stock
1 mg		Pide un presupuesto y un plazo de entrega
5 mg		Pide un presupuesto y un plazo de entrega
10 mg		Pide un presupuesto y un plazo de entrega
25 mg		Pide un presupuesto y un plazo de entrega
50 mg		Pide un presupuesto y un plazo de entrega
100 mg		Pide un presupuesto y un plazo de entrega

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Other Forms of NGD94-1:

NGD 94-1 dimaleate Obtener un presupuesto

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

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Descripciòn

IC₅₀ & Target^[2]

hD_4.2 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.

Peso molecular

320.39

Fòrmula

C₁₈H₂₀N₆

No. CAS

178928-68-2

Appearance

Solid

Color

White to off-white

SMILES

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, protect from light

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

Pureza y Documentación

Purity: 99.73%

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Ficha de datos (272 KB) SDS (252 KB)

COA (247 KB) HNMR (116 KB) LCMS (136 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

NGD94-1 Related Classifications

Neurological Disease

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Help & FAQs

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:

NGD94-1178928-68-2Dopamine Receptordopamine D4 receptorhuman D4.2 receptorfrontostriatalPhencyclidinevervet monkeyInhibitorinhibitorinhibit

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