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Home > Encyclopedia > 6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide structure

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide 

structure
  • CAS No:

    181632-25-7

  • Formula:

    C21H19ClN4O2

  • Chemical Name:

    6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide

  • Synonyms:

    1H-Indole-1-carboxamide,6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-;6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide;SB 242084

  • Categories:

    Pharmaceutical Intermediates  >  Bulk Drug Intermediates

Description

SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, whi


6-chloro-5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-2,3-dihydroindole-1-carboxamide;dihydrochloride is an organic molecular entity, an indole alkaloid and a pyridine. It has a role as a receptor modulator.

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide Basic Attributes

467.775

394.85

DTXSID70394600

Characteristics

67.35000

3.76

white to beige

1.4±0.1 g/cm3

181-183 °C

620.1±55.0 °C at 760 mmHg

328.8±31.5 °C

1.671

DMSO: soluble 15mg/mL, clear

2-8°C

Safety Information

36/37/38

26-36

Xi

6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide Use and Manufacturing

SB 242084 is a 5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. SB 242084 displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors.SB 242084 os a brain penetrant; exerts anxiolytic-like activity.

Computed Properties

Molecular Weight:467.8
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:3
Exact Mass:466.073009
Monoisotopic Mass:466.073009
Topological Polar Surface Area:67.4
Heavy Atom Count:30
Complexity:551
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

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