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Pynegabine

Pharmaceutical compound

Pynegabine

Pynegabine is a Kv7.2 and Kv7.3 potassium channel opener which is under development for the treatment of epilepsy in China. The drug is an analogue of flupirtine and retigabine (ezogabine). However, it shows 55-fold greater potency in activating Kv7.2 channels and 127-fold greater potency in activating Kv7.3 channels compared to retigabine in vitro. In addition, it shows improved chemical or metabolic stability compared to retigabine and in relation to this may have reduced toxicity in comparison. The drug is under development by the Shanghai Institute of Materia Medica and Hainan Haiyao. As of 2026, it is in phase 2 clinical trials for epilepsy.

Pynegabine

Pynegabine
Clinical data
Other namesHN-37
Routes of
administration
Oral[1][2]
Drug classKv7.2 and Kv7.3 potassium channel opener
Identifiers
  • methyl N-[4-[(4-fluorophenyl)methyl-prop-2-ynylamino]-2,6-dimethylphenyl]carbamate
CAS Number
PubChem CID
ChemSpider
ChEMBL
PDB ligand
Chemical and physical data
FormulaC20H21FN2O2
Molar mass340.398 g·mol−1
3D model (JSmol)
  • CC1=CC(=CC(=C1NC(=O)OC)C)N(CC#C)CC2=CC=C(C=C2)F
  • InChI=1S/C20H21FN2O2/c1-5-10-23(13-16-6-8-17(21)9-7-16)18-11-14(2)19(15(3)12-18)22-20(24)25-4/h1,6-9,11-12H,10,13H2,2-4H3,(H,22,24)
  • Key:HXUBJZRAVCPBRH-UHFFFAOYSA-N

Pynegabine (developmental code name HN37) is a Kv7.2 and Kv7.3 potassium channel opener which is under development for the treatment of epilepsy in China.[3][1][2] The drug is an analogue of flupirtine and retigabine (ezogabine).[1][2][4] However, it shows 55-fold greater potency in activating Kv7.2 channels and 127-fold greater potency in activating Kv7.3 channels compared to retigabine in vitro.[1] In addition, it shows improved chemical or metabolic stability compared to retigabine and in relation to this may have reduced toxicity in comparison.[1][2] The drug is under development by the Shanghai Institute of Materia Medica and Hainan Haiyao.[3][1][2] As of 2026, it is in phase 2 clinical trials for epilepsy.[3][1][2]

See also

References

  1. 1 2 3 4 5 6 7 Perucca E, Taglialatela M (March 2025). "Targeting Kv7 Potassium Channels for Epilepsy". CNS Drugs. 39 (3): 263–288. doi:10.1007/s40263-024-01155-3. PMC 11850491. PMID 39853501.
  2. 1 2 3 4 5 6 Pelorosso C, Balestrini S, Guerrini R (May 2026). "Potassium channel agonists emerging as treatment options for focal epilepsy: are we breaking new ground?". Expert Opinion on Emerging Drugs: 1–8. doi:10.1080/14728214.2026.2675274. PMID 42153277.
  3. 1 2 3 "Delving into the Latest Updates on Pynegabine with Synapse". Synapse. 7 March 2026. Retrieved 31 May 2026.
  4. Zhang YM, Xu HY, Hu HN, Tian FY, Chen F, Liu HN, et al. (May 2021). "Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate". Journal of Medicinal Chemistry. 64 (9): 5816–5837. doi:10.1021/acs.jmedchem.0c02252. PMID 33929863.