Ciproxifan

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Ciproxifan
200px
Systematic (IUPAC) name
cyclopropyl 4-(3-(1H-imidazol-4-yl)propyloxy)phenyl ketone
Identifiers
ATC code none
PubChem CID 6422124
IUPHAR/BPS 1265
Chemical data
Formula C16H18N2O2
Molar mass 270.33[[Script error: No such module "String".]]
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Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.

The histamine H3 receptor is an inhibitory autoreceptor located on histaminergic nerve terminals, and is believed to be involved in modulating the release of histamine in the brain. Histamine has an excitatory effect in the brain via H1 receptors in the cerebral cortex, and so drugs such as ciproxifan which block the H3 receptor and consequently allow more histamine to be released have an alertness-promoting effect.[1][2][3]

Ciproxifan produces wakefulness and attentiveness in animal studies, and produced cognitive enhancing effects without prominent stimulant effects at relatively low levels of receptor occupancy, and pronounced wakefulness at higher doses.[4] It has therefore been proposed as a potential treatment for sleep disorders such as narcolepsy and to improve vigilance in old age, particularly in the treatment of conditions such as Alzheimer's disease.[5][6] It also potentiated the effects of antipsychotic drugs, and has been suggested as an adjuvant treatment for schizophrenia.[7]

References

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Psychostimulants, agents used for ADHD, and nootropics (N06B)
Centrally acting sympathomimetics
Xanthine derivatives
Glutamate receptor
CX-516 • CX-546 • CX-614 • CX-691 • CX-717 • IDRA-21 • LY-404,187 • LY-503,430 • PEPA • S-18986 • Sunifiram • Unifiram
Eugeroics / Benzhydryl compounds
Histamine H3 receptor antagonists
A-349,821 • ABT-239 • Ciproxifan • GSK-189,254
GABAA α5 inverse agonists
Dopamine D1 receptor agonists
α7 nicotinic agonists / PAMs
Prolyl endopeptidase inhibitors
Other psychostimulants and nootropics

M: PSO/PSI

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proc, drug(N5A/5B/5C/6A/6B/6D)


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pt:Ciproxifan
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