Bicifadine
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Bicifadine
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CAS No:
71195-57-8
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Formula:
C12H15N
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Chemical Name:
Bicifadine
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Synonyms:
3-Azabicyclo[3.1.0]hexane,1-(4-methylphenyl)-;3-Azabicyclo[3.1.0]hexane,1-(4-methylphenyl)-,(±)-;1-(4-Methylphenyl)-3-azabicyclo[3.1.0]hexane;Bicifadine;1-p-Tolyl-3-aza-bicyclo[3.1.0]hexane;86215-52-3
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CAS No:
Description
Bicifadine (DOV-220075) is a nonopioid analgesic. It is an inhibitor of both the norepinephrine and serotonin transporters and an NMDA antagonist with a non-narcotic profile. Bicifadine was shown to have potent analgesic activity in vivo and was chosen for further development for the treatment of pain.
Characteristics
12
2.18470
1.091g/cm3
204-207 °C @ Solvent: Acetonitrile
276.4ºC at 760 mmHg
125ºC
1.59
Drug Information
For the treatment of pain.
Bicifadine is a chemically distinct molecule with a unique profile of pharmacological activity. Its primary pharmacological action is to enhance and prolong the actions of norepinephrine and serotonin by inhibiting the transport proteins that terminate the physiological actions of the two biogenic amines. Bicifadine is not a narcotic and is well-tolerated and, in preclinical studies, has been shown not to act at any opiate receptor. Bicifadine does not exhibit any anti-inflammatory activity and does not inhibit prostaglandin synthetase in vitro.
The primary enzymes responsible for the primary metabolism of bicifadine in humans are MAO-B and CYP2D6.
Preclinical studies and clinical trials indicate that bicifadine's analgesic properties result through the enhancement and prolongation of norepinephrine and serotonin actions, however other actions may be involved.
bicifadine
Computed Properties
Molecular Weight:173.25
XLogP3:2.1
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:1
Rotatable Bond Count:1
Exact Mass:173.120449483
Monoisotopic Mass:173.120449483
Topological Polar Surface Area:12
Heavy Atom Count:13
Complexity:205
Undefined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes