Iso-THIP

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Iso-THIP
Clinical data
Other namesIsoTHIP; Isogaboxadol
Drug classGABAA-ρ receptor antagonist; GABAA receptor antagonist
ATC code
  • None
Identifiers
  • 4,5,6,7-tetrahydro-1H-[1,2]oxazolo[3,4-c]pyridin-3-one
CAS Number
PubChem CID
ChemSpider
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC6H8N2O2
Molar mass140.142 g·mol−1
3D model (JSmol)
  • C1CNCC2=C1C(=O)ON2
  • InChI=1S/C6H8N2O2/c9-6-4-1-2-7-3-5(4)8-10-6/h7-8H,1-3H2
  • Key:HTKHYLOBQZWEFD-UHFFFAOYSA-N

Iso-THIP, or isoTHIP, is a selective and potent GABAA-ρ receptor (GABAC receptor) antagonist related to gaboxadol (THIP).[1][2][3] It is 4-fold more potent than gaboxadol as a GABAA-ρ receptor antagonist.[2][3] In addition to its GABAA-ρ receptor antagonism, iso-THIP shows much lower but still detectable affinity for the GABAA receptor, where it appears to be an antagonist similarly.[2][3][4] The drug was first described in the scientific literature by Povl Krogsgaard-Larsen and colleagues by 1979.[4][5]

See also

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References

[edit]
  1. ^ Frølund B, Ebert B, Kristiansen U, Liljefors T, Krogsgaard-Larsen P (August 2002). "GABA(A) receptor ligands and their therapeutic potentials". Current Topics in Medicinal Chemistry. 2 (8): 817–832. doi:10.2174/1568026023393525. PMID 12171573.
  2. ^ a b c Johnston GA, Chebib M, Hanrahan JR, Mewett KN (August 2003). "GABA(C) receptors as drug targets". Current Drug Targets. CNS and Neurological Disorders. 2 (4): 260–268. doi:10.2174/1568007033482805. PMID 12871036.
  3. ^ a b c Krehan D, Frølund B, Ebert B, Nielsen B, Krogsgaard-Larsen P, Johnston GA, et al. (November 2003). "Aza-THIP and related analogues of THIP as GABA C antagonists". Bioorganic & Medicinal Chemistry. 11 (23): 4891–4896. doi:10.1016/j.bmc.2003.09.016. PMID 14604650.
  4. ^ a b Krogsgaard-Larsen P, Mikkelsen H, Jacobsen P, Falch E, Curtis DR, Peet MJ, et al. (June 1983). "4,5,6,7-Tetrahydroisothiazolo[5,4-c]pyridin-3-ol and related analogues of THIP. Synthesis and biological activity". Journal of Medicinal Chemistry. 26 (6): 895–900. doi:10.1021/jm00360a020. PMID 6304315.
  5. ^ Arnt J, Krogsgaard-Larsen P (November 1979). "GABA agonists and potential antagonists related to muscimol". Brain Research. 177 (2): 395–400. doi:10.1016/0006-8993(79)90793-5. PMID 227538.
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