GAL-021

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]

GAL-021
Clinical data
Routes of
administration
IV
ATC code
  • None
Legal status
Legal status
Identifiers
IUPAC name
  • 2-[(N-Methyl-N-methoxy)amino]-4,6-bis(propylamino)-1,3,5-triazine
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC11H22N6O
Molar mass254.338 g·mol−1
3D model (JSmol)
SMILES
  • CCCNc1nc(nc(N(C)OC)n1)NCCC

See also

References

  1. 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". British Journal of Anaesthesia. 113 (5): 875–83. doi:10.1093/bja/aeu182. PMID 24989775.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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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