ENA-001

ENA-001
Clinical data
Routes of; administration	IV
ATC code	None;
Legal status
Legal status	US: Investigational New Drug;
Identifiers
	IUPAC name 2-[(N-Methyl-N-methoxy)amino]-4,6-bis(propylamino)-1,3,5-triazine;
CAS Number	1380341-99-0;
PubChem CID	57340959;
ChemSpider	62866096;
UNII	4RZ4OGT40Z;
CompTox Dashboard (EPA)	DTXSID601031220 ;
Chemical and physical data
Formula	C11H22N6O
Molar mass	254.338 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCCNc1nc(nc(N(C)OC)n1)NCCC;
	InChI 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 BK_Ca 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]

References

^ 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.
^ 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.
^ 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.
^ 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.
^ 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.
^ 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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[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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v t e Other respiratory system products (R07)
Lung surfactants	Colfosceril palmitate Dipalmitoylphosphatidylcholine
Respiratory stimulants	Almitrine Amiphenazole Bemegride Dimefline Doxapram Etamivan GAL-021 Mepixanox Nikethamide Pentetrazol Prethcamide
5-HT4 receptor agonists	BIMU-8 Zacopride
Other agents for treating respiratory depression	Ivacaftor (+ lumacaftor, + tezacaftor, + elexacaftor/tezacaftor) Nitric oxide BW373U86 CX-546 CX-717

See also

References