Ciproxifan – An Essential Type of Histamine Inhibitor

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Ciproxifan, or cyclopropyl-(4-(3-1H-imidazol-4-yl)propyloxy) phenyl) ketone, is a novel compound belonging to a group of H3-receptor agonists. It is observed to be highly potent in current animal studies, which means that being a H3-receptor agonist, Ciproxifan has a very promising potential for medical and therapeutic use as a waking and a cognitive enhancing agent. Ciproxifan was also observed in animal studies to have the ability to enhance attention and vigilance, thus making also a potential treatment and management option for neurological disorders associated with old age.

H3-receptor is essentially a type of histamine inhibitor. Histamine is a compound that figures in immune system response and is also a type of neurotransmitter. As a neurotransmitter, the levels of histamine can modulate sleeping patterns as high levels of it can increase wakefulness and prevent sleep. This is why some antihistamine type drugs that are usually prescribed as a treatment for allergy cause drowsiness and induce sleep.

Histamine

Researchers classify Ciproxifan as a wakefulness promoting agent, similar to Modafinil and Armodafinil but with a different mechanism of action. Ciproxifan blocks the H3-receptors allowing more histamine to be released in the brain. Wakefulness, along with vigilance and alertness is induced as the levels of histamine in the brain are increased. This ability gives Ciproxifan a good potential of becoming yet another therapeutic alternative for sleep disorders such as narcolepsy, shift work sleep disorder, and obstructive sleep apnea.

One of the creators of Ciproxifan is Dr. Michel Jouvet, a famous French neurological scientist. Dr. Jouvet is a multi-awarded researcher and one of his main claims to fame is being the first researcher who developed Modafinil.

The histaminergic system of the central nervous system plays a major role in the sleep-wake cycles of an individual and the direct effect of Ciproxifan on histamines adds to its potency and effectiveness as a wakefulness enhancing agent.  The laboratory animals that were artificially induced with sleepiness appeared to have recovered a nearly total waking state after an oral administration of Ciproxifan. This same study also affirms other observations that Ciproxifan has a very high bioavailability and that it can cross the blood-brain barrier quite easily.

While it is not directly observed in the studies, Ciproxifan appears to also have nootropic properties as the rats in some of the studies were observed to have increased ability in completing tasks that required memory and analytical processes.  Ciproxifan was also suggested in some studies to be a potential anti-psychotic agent, particularly for the treatment and cure for schizophrenia. In a study conducted in 2002, it was observed that Ciproxifan potentiates the neurochemical and behavioral effects of Haloperidol in laboratory mice.

Although Ciproxifan have produced generally positive results in its initial animal studies, there were also a few negative aspects of the compound that were observed. In a comparative study done on with Ciproxifan, which is an imidazole-based compound was compared with the non-imidazole drug Methylphenidate. The results of the study showed that the rats treated with Ciproxifan developed a tolerance for the compound after 10 to 15 days. Tolerance may be able to be avoided with cycling, but there are currently no data available on this at the moment.

PROS

  1. It appears to be a potent and an effective wakefulness promoting agent.
  2. It appears to have cognitive enhancing effects.
  3. It has high bioavailability even when taken orally and can cross the blood-brain barrier easily.
  4. It has a good potential as treatment for various neurological conditions.

CONS

  1. Studies show that one can develop a tolerance for it.
  2. It hasn’t been tested on humans yet.
  3. Acquiring it now through independent labs is very expensive.

At this stage of the studies and trials on Ciproxifan, analog derivatives of the compound are being developed in order to maximize its potential as well as address some of its negative properties. It must be noted that this compound has yet to be tested on humans, so whether or not it is deemed as fit and safe for therapeutic purposes remains to be seen.

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