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Cat. No.: HY-165450

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NNC-112

NNC-112 is a dopamine D1 receptor antagonist with a K_i of 0.18 nM for rat D1R and a K_i of 18 nM for 5-HT2. NNC-112 competitively inhibits [³H]SCH 23390 binding and blocks dopamine-stimulated adenylate cyclase. NNC-112 blocks D1 receptor-mediated rotational behavior in 6-OHDA-lesioned rats. NNC-112 can serve as a C11-labeled radioligand ([11C] NNC 112) for positron emission tomography imaging. NNC-112 can be used for research on schizophrenia and hypertension.

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CAS No.: 125341-24-4
Formule: C₁₉H₁₈ClNO₂
Masse moléculaire:327.81

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Please store the product under the recommended conditions in the Certificate of Analysis.

NNC-112 Chemical Structure

CAS No.: 125341-24-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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- IC₅₀ & Target
- In Vitro
- In Vivo
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Description

IC₅₀ & Target

^[2]

D₁ Receptor

0.18 nM (Ki)

5-HT_2A Receptor

18 nM (Ki)

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In Vitro

NNC-112 (60 min) is a highly potent inhibitor of the binding of [³H]SCH 23390 to rat striatal dopamine D₁ receptors, with a K_I of 0.18 nM^[2].
NNC-112 (20 min) exhibits low affinity for rat striatal dopamine D₂ receptors, with a K_I of 898 nM^[2].
NNC-112 exhibits moderate affinity for 5-HT₂ receptors with a K_I of 18 nM^[2].
NNC-112 (15 min) is a potent competitive inhibitor of dopamine-stimulated adenylate cyclase in rat striatal tissue, with a K_I of 2.8 nM^[2].

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

In Vivo

NNC-112 (s.c.; 0.5 h before sacrifice) is a potent and selective inhibitor of D₁ receptor binding in mice, with an ED₅₀ of 0.015 mg/kg, and shows no activity at D₂ receptors^[2].
NNC-112 (s.c.; 0.5 h before the agonist) selectively antagonizes D₁ receptor-mediated rotational behavior in 6-OHDA (HY-B1081A)-lesioned rats with an ED₅₀ of 0.08 mg/kg, without affecting D₂-mediated rotation^[2].
Pretreatment with NNC-112 (2-2.5 mg/kg; i.v.) produces 77% blockade of [¹¹C]NNC 112 binding in the rat renal cortex, indicating that the PET signal is predominantly driven by specific D₁-like receptor binding^[4].

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

Animal Model:

Sprague-Dawley rats^[4]
Dosage:

2 mg/kg; 2.5 mg/kg
Administration:

i.v.; single pretreatment bolus
Result:

Reached an average of 0.083% injected dose per mL of tissue at 35 min in the left renal cortex, corresponding to a blocking percentage of 77%.

Related Protocols :

Research Protocol for Cardiovascular Diseases

Chemical Information

CAS No. 125341-24-4
Masse moléculaire 327.81
Formule C₁₉H₁₈ClNO₂
SMILES

CN1C[C@@H](C=2C(=CC(Cl)=C(O)C2)CC1)C3=C4C(=CC=C3)C=CO4
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Verma M. Evaluating a Positive Allosteric Modulator Radiotracer Candidate to Image the Dopamine D1 Receptor (Doctoral dissertation, Université d'Ottawa| University of Ottawa).

[2]. Andersen PH, et al. NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists. European journal of pharmacology. 1992 Aug 14;219(1):45-52. [Content Brief]

[3]. Sedvall GC, et al. Pharmacological manipulation of D1-dopamine receptor function in schizophrenia. Neuropsychopharmacology. 1999 Dec 1;21(6):S181-8.

[4]. Granda ML, et al. First D1-like receptor PET imaging of the rat and primate kidney: implications for human disease monitoring. American journal of physiology. Renal physiology. 2014 Jul 01;307(1):F116-21.

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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NNC-112

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