ENA-001 explained

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

Notes and References

  1. Miller TL, Raab LM, Shaffer TH, Schweikert A, Diana F, Fort P, Frum AS, Pergolizzi J, Raffa RB . 6 . A Novel Agnostic Respiratory Stimulant as a Treatment for Apnea of Prematurity: A Proof-of-Concept Study . Cureus . 14 . 9 . e28900 . September 2022 . 36237747 . 10.7759/cureus.28900 . free . 9544529 . 252141895 .
  2. McLeod JF, Leempoels JM, Peng SX, Dax SL, Myers LJ, Golder FJ . 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 . November 2014 . 24989775 . 10.1093/bja/aeu182 . free .
  3. Baby SM, Hoshi T, Peng S, Dax SL, Golder FJ, MacIntyre DE, Mannion JC . Comparison of the respiratory effects of GAL-021 in BK α subunit knockout (Slo1−/−) and wild-type mice . The FASEB Journal . 2012 . 26 . 1 Supplement . 704.30 . 10.1096/fasebj.26.1_supplement.704.30 . free .
  4. Golder FJ, Hewitt MM, McLeod JF . Respiratory stimulant drugs in the post-operative setting . Respiratory Physiology & Neurobiology . 189 . 2 . 395–402 . November 2013 . 23791825 . 10.1016/j.resp.2013.06.010 . 2558991 . free .
  5. Baby SM, Gruber RB, Puskovic V, Peng S, Dax SL, Golder FJ, MacIntyre DE, Mannion JC . GAL-021, a novel respiratory stimulant, attenuates opioid–induced respiratory depression without compromising analgesia . The FASEB Journal . 2012 . 26 . 1 Supplement . 704.28 . 10.1096/fasebj.26.1_supplement.704.28. free .
  6. van der Schier R, Roozekrans M, van Velzen M, Dahan A, Niesters M . Opioid-induced respiratory depression: reversal by non-opioid drugs . F1000Prime Reports . 6 . 79 . 4 September 2014 . 25343036 . 4173639 . 10.12703/P6-79 . free .
  7. Roozekrans M, van der Schrier R, Okkerse P, Hay J, McLeod JF, Dahan A . Two studies on reversal of opioid-induced respiratory depression by BK-channel blocker GAL021 in human volunteers . Anesthesiology . 121 . 3 . 459–468 . September 2014 . 25222672 . 10.1097/ALN.0000000000000367 . 35738816 . free .

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