125341-24-4
Chemical Structure
NNC-112
- CAS No.: 125341-24-4
- Formula:C19H18ClNO2
- Molecular Weight:327.81
IUPAC Name: (S)-5-(benzofuran-7-yl)-8-chloro-3-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol
InChIKey: RUSANBIFMAXXSJ-MRXNPFEDSA-N
SMILES: CN1C[C@@H](C=2C(=CC(Cl)=C(O)C2)CC1)C3=C4C(=CC=C3)C=CO4
Biological Activity: 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[1][2][3][4].
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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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References
- [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.
