ENA-001
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| Routes of administration | IV |
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| Formula | C11H22N6O |
| Molar mass | 254.338 g·mol−1 |
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GAL-021 is a drug related to almitrine which acts as a respiratory stimulant, with its mechanism of action primarily thought to involve blocking the BKCa potassium channel,[1] although secondary mechanisms may also be involved.[2] It was developed by Galleon Pharmaceuticals, and is being tested in clinical trials for potential uses in post-operative care,[3] as well as more generally to counteract the respiratory depression which can be a side effect of opioid analgesic drugs.[4][5][6]
See also
References
- ^ McLeod JF, Leempoels JM, Peng SX, Dax SL, Myers LJ, Golder FJ (November 2014). "GAL-021, a new intravenous BKCa-channel blocker, is well tolerated and stimulates ventilation in healthy volunteers" (PDF). British Journal of Anaesthesia. 113 (5): 875–83. doi:10.1093/bja/aeu182. PMID 24989775.
- ^ Baby SM, Hoshi T, Peng S, Dax SL, Golder FJ, MacIntyre DE, Mannion JC (2012). "Comparison of the respiratory effects of GAL-021 in BK α subunit knockout (Slo1−/−) and wild-type mice". The FASEB Journal. 26 (1 Supplement): 704.30. doi:10.1096/fasebj.26.1_supplement.704.30 (inactive 2021-01-10).
{{cite journal}}: CS1 maint: DOI inactive as of January 2021 (link) CS1 maint: unflagged free DOI (link) - ^ Golder FJ, Hewitt MM, McLeod JF (November 2013). "Respiratory stimulant drugs in the post-operative setting". Respiratory Physiology & Neurobiology. 189 (2): 395–402. doi:10.1016/j.resp.2013.06.010. PMID 23791825. S2CID 2558991.
- ^ Baby SM, Gruber RB, Puskovic V, Peng S, Dax SL, Golder FJ, MacIntyre DE, Mannion JC (2012). "GAL-021, a novel respiratory stimulant, attenuates opioid–induced respiratory depression without compromising analgesia". The FASEB Journal. 26 (1 Supplement): 704.28. doi:10.1096/fasebj.26.1_supplement.704.28 (inactive 2021-01-10).
{{cite journal}}: CS1 maint: DOI inactive as of January 2021 (link) CS1 maint: unflagged free DOI (link) - ^ van der Schier R, Roozekrans M, van Velzen M, Dahan A, Niesters M (4 September 2014). "Opioid-induced respiratory depression: reversal by non-opioid drugs". F1000prime Reports. 6: 79. doi:10.12703/P6-79. PMC 4173639. PMID 25343036.
{{cite journal}}: CS1 maint: unflagged free DOI (link) - ^ Roozekrans M, van der Schrier R, Okkerse P, Hay J, McLeod JF, Dahan A (September 2014). "Two studies on reversal of opioid-induced respiratory depression by BK-channel blocker GAL021 in human volunteers". Anesthesiology. 121 (3): 459–68. doi:10.1097/ALN.0000000000000367. PMID 25222672. S2CID 35738816.
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