Chemistry:Aza-THIP

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Aza-THIP is a selective and moderately potent GABAA-ρ (GABAC receptor) antagonist related to gaboxadol (THIP).[1][2][3][4] Unlike gaboxadol, it is virtually inactive at the GABAA receptor.[1][2][4][5] The drug was first described in the scientific literature by Povl Krogsgaard-Larsen and colleagues by 1979.[6][7]

See also

  • Thio-THIP
  • Iso-THIP
  • THAZ

References

  1. ↑ 1.0 1.1 "GABAA Agonists and Partial Agonists: THIP (Gaboxadol) as a Non-Opioid Analgesic and a Novel Type of Hypnotic1". GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic. Advances in Pharmacology. 54. 2006. pp. 53–71. doi:10.1016/s1054-3589(06)54003-7. ISBN 978-0-12-032957-1. 
  2. ↑ 2.0 2.1 "GABA(C) receptors as drug targets". Current Drug Targets. CNS and Neurological Disorders 2 (4): 260–268. August 2003. doi:10.2174/1568007033482805. PMID 12871036. 
  3. ↑ "Neurochemicals for the investigation of GABA(C) receptors". Neurochemical Research 35 (12): 1970–1977. December 2010. doi:10.1007/s11064-010-0271-7. PMID 20963487. 
  4. ↑ 4.0 4.1 "Aza-THIP and related analogues of THIP as GABA C antagonists". Bioorganic & Medicinal Chemistry 11 (23): 4891–4896. November 2003. doi:10.1016/j.bmc.2003.09.016. PMID 14604650. 
  5. ↑ "GABA(A) receptor ligands and their therapeutic potentials". Current Topics in Medicinal Chemistry 2 (8): 817–832. August 2002. doi:10.2174/1568026023393525. PMID 12171573. 
  6. ↑ "GABA agonists. Development and interactions with the GABA receptor complex". Molecular and Cellular Biochemistry 38 Spec No (Pt 1): 129–146. August 1981. doi:10.1007/BF00235692. PMID 6270544. 
  7. ↑ "GABA agonists. Synthesis and structure-activity studies on analogs of isoguvacine and THIP.". Chimica Therapeutica (European Journal of Medicinal Chemistry) 14: 157–164. 1979. 

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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

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