ENA-001

Last updated
ENA-001
GAL-021.svg
Clinical data
Routes of
administration 		IV
ATC code
  • None
Legal status
Legal status
Identifiers
  • 2-[(N-Methyl-N-methoxy)amino]-4,6-bis(propylamino)-1,3,5-triazine
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C11H22N6O
Molar mass 254.338 g·mol−1
3D model (JSmol)
  • CCCNc1nc(nc(N(C)OC)n1)NCCC
  • InChI=1S/C11H22N6O/c1-5-7-12-9-14-10(13-8-6-2)16-11(15-9)17(3)18-4/h5-8H2,1-4H3,(H2,12,13,14,15,16)
  • Key:FJNLCHNQVJVCPY-UHFFFAOYSA-N

ENA-001 (formerly GAL-021) [1] 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, [2] although secondary mechanisms may also be involved. [3] It was developed by Galleon Pharmaceuticals, and is being tested in clinical trials for potential uses in post-operative care, [4] as well as more generally to counteract the respiratory depression which can be a side effect of opioid analgesic drugs. [5] [6] [7]

See also

References

  1. ↑ Miller TL, Raab LM, Shaffer TH, Schweikert A, Diana F, Fort P, et al. (September 2022). "A Novel Agnostic Respiratory Stimulant as a Treatment for Apnea of Prematurity: A Proof-of-Concept Study". Cureus. 14 (9) e28900. doi: 10.7759/cureus.28900 . PMC   9544529 . PMID   36237747. S2CID   252141895.
  2. ↑ 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): 875–883. doi: 10.1093/bja/aeu182 . PMID   24989775.
  3. ↑ 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 .
  4. ↑ 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.
  5. ↑ 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 .
  6. ↑ 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.
  7. ↑ 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): 459–468. doi: 10.1097/ALN.0000000000000367 . PMID   25222672. S2CID   35738816.
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