Identification
Name Guvacine
Accession Number DB08848
Type small molecule
Description Guvacine is a pyridine alkaloid found in the Areca nut (also known as the Betel nut). It is an experimental drug with no approved indication. Experimental studies are still being investigated to determine all of the physiological effects and mechanisms of action of guvacine. Currently it has been determined that guvacine is a specific GABA reuptake inhibitor with no significant affinity at GABA receptors.
Structure
Categories (*)
Molecular Weight 127.1412
Groups experimental
Monoisotopic Weight 127.063328537
Pharmacology
Indication There is no approved indication for guvacine.
Mechanism of action Experimental studies are still being investigated to determine the exact mechanisms of action of guvacine. What is known is that guvacine binds selectively to presynaptic GABA reuptake transporters and prevents the reuptake of GABA, but has no affinity for GABA postsynaptic receptors.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions Not Available
Food Interactions Not Available
Sodium- and chloride-dependent GABA transporter 2
Name Sodium- and chloride-dependent GABA transporter 2
Gene Name Not Available
Pharmacological action unknown
Actions inhibitor
References
  • Schousboe A, Thorbek P, Hertz L, Krogsgaard-Larsen P: Effects of GABA analogues of restricted conformation on GABA transport in astrocytes and brain cortex slices and on GABA receptor binding. J Neurochem. 1979 Jul;33(1):181-9. - Pubmed
  • Krogsgaard-Larsen P, Frolund B, Frydenvang K: GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Curr Pharm Des. 2000 Aug;6(12):1193-209. - Pubmed
  • Sunol C, Babot Z, Cristofol R, Sonnewald U, Waagepetersen HS, Schousboe A: A possible role of the non-GAT1 GABA transporters in transfer of GABA from GABAergic to glutamatergic neurons in mouse cerebellar neuronal cultures. Neurochem Res. 2010 Sep;35(9):1384-90. doi: 10.1007/s11064-010-0196-1. Epub 2010 May 30. - Pubmed
DTHybrid score Not Available
Sodium- and chloride-dependent GABA transporter 1
Name Sodium- and chloride-dependent GABA transporter 1
Gene Name SLC6A1
Pharmacological action unknown
Actions inhibitor
References
  • Sunol C, Babot Z, Cristofol R, Sonnewald U, Waagepetersen HS, Schousboe A: A possible role of the non-GAT1 GABA transporters in transfer of GABA from GABAergic to glutamatergic neurons in mouse cerebellar neuronal cultures. Neurochem Res. 2010 Sep;35(9):1384-90. doi: 10.1007/s11064-010-0196-1. Epub 2010 May 30. - Pubmed
DTHybrid score 0.7969
Sodium- and chloride-dependent GABA transporter 3
Name Sodium- and chloride-dependent GABA transporter 3
Gene Name Not Available
Pharmacological action unknown
Actions inhibitor
References
  • Sunol C, Babot Z, Cristofol R, Sonnewald U, Waagepetersen HS, Schousboe A: A possible role of the non-GAT1 GABA transporters in transfer of GABA from GABAergic to glutamatergic neurons in mouse cerebellar neuronal cultures. Neurochem Res. 2010 Sep;35(9):1384-90. doi: 10.1007/s11064-010-0196-1. Epub 2010 May 30. - Pubmed
DTHybrid score Not Available
Sodium- and chloride-dependent betaine transporter
Name Sodium- and chloride-dependent betaine transporter
Gene Name Not Available
Pharmacological action unknown
Actions inhibitor
References
  • Ruiz-Tachiquin ME, Sanchez-Lemus E, Soria-Jasso LE, Arias-Montano JA, Ortega A: Gamma-aminobutyric acid transporter (BGT-1) expressed in human astrocytoma U373 MG cells: pharmacological and molecular characterization and phorbol ester-induced inhibition. J Neurosci Res. 2002 Jul 1;69(1):125-32. - Pubmed
DTHybrid score Not Available