NNC-112
NNC-112 is a dopamine D1 receptor antagonist with a Ki of 0.18 nM for rat D1R and a Ki 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
- 화학식: C19H18ClNO2
- 분자량:327.81
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[2]|
D1 Receptor 0.18 nM (Ki) |
5-HT2A Receptor 18 nM (Ki) |
In Vitro
NNC-112 (20 min) exhibits low affinity for rat striatal dopamine D2 receptors, with a KI of 898 nM[2].
NNC-112 exhibits moderate affinity for 5-HT2 receptors with a KI of 18 nM[2].
NNC-112 (15 min) is a potent competitive inhibitor of dopamine-stimulated adenylate cyclase in rat striatal tissue, with a KI 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 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.
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Animal Model:Sprague-Dawley rats[4]
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Dosage:2 mg/kg; 2.5 mg/kg
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Administration:i.v.; single pretreatment bolus
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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%.
Chemical Information
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CAS No. 125341-24-4
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분자량 327.81
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화학식 C19H18ClNO2
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SMILES
CN1C[C@@H](C=2C(=CC(Cl)=C(O)C2)CC1)C3=C4C(=CC=C3)C=CO4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NNC-112 Related Classifications
HY-165450 Related Classifications
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