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BIMU8

BIMU8

IUPAC name	endo-N-8- methyl-8- azabicyclo[3.2.1] oct-3-yl)- 2,3-dihydro-3- isopropyl-2-oxo- 1H-benzimidazol-1-carboxamide hydrochloride
Identifiers
CAS number	134296-40-5
PubChem	5311028
Properties
Molecular formula	C19H27ClN4O2
Molar mass	378.896
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) Infobox disclaimer and references

BIMU-8 is a novel compound which acts on an area of the brain stem known as the pre-Botzinger complex.

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Explanation

The pre-Botzinger complex has been found to drive respiration. BIMU-8 stimulates this area of the brain, causing an increase in the rate of respiration. BIMU-8 acts as a selective 5HT₄ agonist and is one of the first compounds to be developed that was selective for this serotonin receptor subtype.

Practical use of BIMU-8

The most obvious practical use of BIMU-8 is to combine it with opiates in order to counteract the dangerous respiratory depressing properties of the latter.^[1] BIMU-8 does not affect the painkilling properties of opiates, which means that if combined with BIMU-8, large therapeutic doses of opiates could theoretically be given to humans without risking a decrease in breathing rate. Studies have shown BIMU-8 to be effective in rats at counteracting the respiratory depression caused by the potent opioid fentanyl, which has caused many accidental deaths in humans. However no human trials of BIMU-8 have yet been carried out.

Other studies have suggested a role for 5HT₄ agonists in learning and memory,^[2] BIMU-8 was found to increase conditioned responses in mice, and so this drug might also be useful for improving memory in humans. Interestingly other selective 5HT₄ agonists such as mosapride (the only 5HT₄ agonist currently available for use in humans) have been found not to reduce respiratory depression,^[3] suggesting that BIMU-8 may affect 5HT₄ receptors in a different way to other 5HT₄ agonists, or alternatively that the anti-respiratory depressant effect of BIMU-8 is instead mediated through a different mechanism of action which has not yet been elucidated.

References

^ Manzke T, Guenther U, Ponimaskin E, Haller M, Dutschmann M, Schwarzacher S, Richter D (2003). "5-HT4(a) receptors avert opioid-induced breathing depression without loss of analgesia". Science 301 (5630): 226-9. PMID 12855812.
^ Meneses A, Hong E (1997). "Effects of 5-HT4 receptor agonists and antagonists in learning". Pharmacol Biochem Behav 56 (3): 347-51. PMID 9077568.
^ Lotsch J, Skarke C, Schneider A, Hummel T, Geisslinger G. The 5-hydroxytryptamine 4 receptor agonist mosapride does not antagonize morphine-induced respiratory depression. Clinical Pharmacology and Therapeutics. 2005 Sep;78(3):278-87.

Categories: Respiratory agents | Nitrogen heterocycles | Antidotes | Serotonin receptor agonists

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "BIMU8". A list of authors is available in Wikipedia.