BIMU8
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BIMU8
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| Systematic (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 | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C19H26N4O2 |
| Mol. mass | 342.44 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
BIMU-8 is a 5-HT4 receptor selective agonist. BIMU-8 was one of the first compounds of this class. BIMU-8 also increases in the rate of respiration by activating an area of the brain stem known as the pre-Botzinger complex, possibly through an unknown mechanism.
[edit] Use
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,[2] 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,[3] 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 and tegaserod (the only 5HT4 agonists currently available for use in humans) have been found not to reduce respiratory depression,[4] 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.
[edit] 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. doi:. PMID 12855812.
- ^ Wang X, Dergacheva O, Kamendi H, Gorini C, Mendelowitz D. 5-Hydroxytryptamine 1A/7 and 4alpha receptors differentially prevent opioid-induced inhibition of brain stem cardiorespiratory function. Hypertension. 2007 Aug;50(2):368-76. PMID 17576856
- ^ Meneses A, Hong E (1997). "Effects of 5-HT4 receptor agonists and antagonists in learning". Pharmacol Biochem Behav 56 (3): 347–51. doi:. 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.
[edit] External links
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