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Tezampanel

Chemical compound

Chemical compound

Tezampanel (, ) (developmental code names LY-293,558, LY-326,325, NGX-424) is a drug originally developed by Eli Lilly which acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective and anticonvulsant properties, the former of which may, at least in part, occur via blockade of calcium uptake into neurons.

Tezampanel has a range of effects which may be useful for medicinal purposes, as well as its applications in scientific research. It suppresses both the withdrawal symptoms from morphine and other opioids, and the development of tolerance, as well as having antihyperalgesic and analgesic effects in its own right. It also has anxiolytic effects in animal studies and has been suggested as a candidate for the treatment of anxiety in humans.

Whereas tezampanel free base is known as LY-293558, tezampanel hydrochloride is said to be known as LY-326325.

References

References

  1. (September 2001). "LY-293558. Eli Lilly & Co". Current Opinion in Investigational Drugs.
  2. (July 1993). "(3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3 - carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist". Journal of Medicinal Chemistry.
  3. (September 1995). "In vitro and in vivo antagonism of AMPA receptor activation by (3S, 4aR, 6R, 8aR)-6-[2-(1(2)H-tetrazole-5-yl) ethyl] decahydroisoquinoline-3-carboxylic acid". Neuropharmacology.
  4. (April 1996). "Pharmacological discrimination of GluR5 and GluR6 kainate receptor subtypes by (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)ethyl]decahyd roisdoquinoline-3 carboxylic-acid". Molecular Pharmacology.
  5. (1998). "GluR5 kainate receptor mediated synaptic transmission in rat basolateral amygdala in vitro". Neuropharmacology.
  6. (May 1994). "Neuroprotective effect of the AMPA receptor antagonist LY-293558 in focal cerebral ischemia in the cat". Journal of Cerebral Blood Flow and Metabolism.
  7. (2001). "Role of AMPA and GluR5 kainate receptors in the development and expression of amygdala kindling in the mouse". Neuropharmacology.
  8. (November 1995). "Effects of decahydroisoquinoline-3-carboxylic acid monohydrate, a novel AMPA receptor antagonist, on glutamate-induced CA2+ responses and neurotoxicity in rat cortical and cerebellar granule neurons". Biochemical Pharmacology.
  9. (November 1996). "A selective AMPA antagonist, LY293558, suppresses morphine withdrawal-induced activation of locus coeruleus neurons and behavioral signs of morphine withdrawal". Neuropsychopharmacology.
  10. (December 1997). "The competitive alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist LY293558 attenuates and reverses analgesic tolerance to morphine but not to delta or kappa opioids". The Journal of Pharmacology and Experimental Therapeutics.
  11. (December 1997). "The effects of LY293558, an AMPA receptor antagonist, on acute and chronic morphine dependence". Brain Research.
  12. (March 1999). "AMPA antagonist LY293558 blocks the development, without blocking the expression, of behavioral sensitization to morphine". Synapse.
  13. (November 1998). "AMPA/kainate antagonist LY293558 reduces capsaicin-evoked hyperalgesia but not pain in normal skin in humans". Anesthesiology.
  14. (September 2000). "Effects of the 2-amino-3-hydroxy-5-methyl-4-isoxazole-proprionic acid/kainate antagonist LY293558 on spontaneous and evoked postoperative pain". Clinical Pharmacology and Therapeutics.
  15. (July 2002). "Effect of intrathecal non-NMDA EAA receptor antagonist LY293558 in rats: a new class of drugs for spinal anesthesia". Anesthesiology.
  16. (July 2004). "LY293558, a novel AMPA/GluR5 antagonist, is efficacious and well-tolerated in acute migraine". Cephalalgia.
  17. (October 2006). "The effect of the AMPA/kainate receptor antagonist LY293558 in a rat model of postoperative pain". The Journal of Pain.
  18. (October 2007). "Epidural tezampanel, an AMPA/kainate receptor antagonist, produces postoperative analgesia in rats". Anesthesia and Analgesia.
  19. (April 2006). "In vitro and in vivo studies in rats with LY293558 suggest AMPA/kainate receptor blockade as a novel potential mechanism for the therapeutic treatment of anxiety disorders". Psychopharmacology.
  20. (February 2011). "Medicinal chemistry of competitive kainate receptor antagonists". ACS Chem Neurosci.
  21. (2002). "Kainate receptor agonists, antagonists and allosteric modulators". Curr Pharm Des.
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ampa-receptor-antagonists analgesics anticonvulsants antimigraine-drugs carboxylic-acids decahydroisoquinolines drugs-developed-by-eli-lilly-and-company kainate-receptor-antagonists neuroprotective-agents tetrazoles
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