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Тезампанел LY 293 55 лікарський засіб розроблений фармацевтичною компанією Eli Lilly Механізм дії полягає в антагонізмі

Тезампанел

Тезампанел

Тезампанел (LY-293,55) — лікарський засіб, розроблений фармацевтичною компанією Eli Lilly. Механізм дії полягає в антагонізмі ефектів АМРА- та каїнатних рецепторів, з більш високою афінністю до субодиниці GluR5 каїнатного рецептора. Препарату притаманна та дія. Механізм нейропротекторного впливу на ЦНС полягає, щонайменше частково, в блокуванні транспорту кальцію всередину нейронів.

Тезампанел
image
Систематична назва (IUPAC)
(3S,4aR,6R,8aR)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid
Ідентифікатори
Номер CAS 150131-78-5
Код ATC
PubChem 127894
Хімічні дані
Формула C13H21N5O2 
Мол. маса 279,338 г/моль
SMILES eMolecules & PubChem
Фармакокінетичні дані
Біодоступність ?
Метаболізм ?
Період напіврозпаду ?
Виділення ?
Терапевтичні застереження
Кат. вагітності

?

Дозволений для наукових досліджень

Шляхи введення ?

Тезампанел має також значну кількість ефектів, потенційно придатних як для терапевтичного використання, так і для використання в наукових дослідженнях. Він полегшує абстинентний синдром від морфіну та інших опіоїдів, а також істотно гальмує розвиток звикання до них. Окрім того, тезампанел виявляє антигіперанальгетичні та анальгетичні ефекти. Окрім того, при дослідах на тваринах дана речовина показала анксіолітичні властивості, в результаті чого була рекомендована для використання як анксіолітик для людей.

Література

  1. Gilron I. LY-293558. Eli Lilly & Co. Current Opinion in Investigational Drugs. 2001 Sep;2(9):1273-8. PMID 11717815
  2. Ornstein PL, Arnold MB, Augenstein NK, Lodge D, Leander JD, Schoepp DD. (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. 1993 Jul 9;36(14):2046-8. PMID 8393116
  3. Schoepp DD, Lodge D, Bleakman D, Leander JD, Tizzano JP, Wright RA, Palmer AJ, Salhoff CR, Ornstein PL. 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. 1995 Sep;34(9):1159-68. PMID 8532186
  4. Bleakman R, Schoepp DD, Ballyk B, Bufton H, Sharpe EF, Thomas K, Ornstein PL, Kamboj RK. 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. 1996 Apr;49(4):581-5. PMID 8609884
  5. Li H, Rogawski MA. GluR5 kainate receptor mediated synaptic transmission in rat basolateral amygdala in vitro. Neuropharmacology. 1998Oct-Nov;37(10-11):1279-86. PubMed PMID 9849665.
  6. Bullock R, Graham DI, Swanson S, McCulloch J. Neuroprotective effect of the AMPA receptor antagonist LY-293558 in focal cerebral ischemia in the cat. Journal of Cerebral Blood Flow and Metabolism. 1994 May;14(3):466-71. PMID 8163588
  7. Rogawski MA, Kurzman PS, Yamaguchi SI, Li H. Role of AMPA and GluR5 kainate receptors in the development and expression of amygdala kindling in the mouse. Neuropharmacology. 2001;40(1):28-35. PubMed PMID 11077068.
  8. Liljequist S, Cebers G, Kalda A. 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. 1995 Nov 27;50(11):1761-74. PMID 8615854
  9. Rasmussen K, Kendrick WT, Kogan JH, Aghajanian GK. A selective AMPA antagonist, LY293558, suppresses morphine withdrawal-induced activation of locus coeruleus neurons and behavioral signs of morphine withdrawal. Neuropsychopharmacology. 1996 Nov;15(5):497-505. PMID 8914123
  10. Kest B, McLemore G, Kao B, Inturrisi CE. 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. Journal of Pharmacology and Experimental Therapeutics. 1997 Dec;283(3):1249-55. PMID 9400000
  11. McLemore GL, Kest B, Inturrisi CE. The effects of LY293558, an AMPA receptor antagonist, on acute and chronic morphine dependence. Brain Research. 1997 Dec 5;778(1):120-6. PMID 9462883
  12. Carlezon WA Jr, Rasmussen K, Nestler EJ. AMPA antagonist LY293558 blocks the development, without blocking the expression, of behavioral sensitization to morphine. Synapse. 1999 Mar 15;31(4):256-62. PMID 10051106
  13. Sang CN, Hostetter MP, Gracely RH, Chappell AS, Schoepp DD, Lee G, Whitcup S, Caruso R, Max MB. AMPA/kainate antagonist LY293558 reduces capsaicin-evoked hyperalgesia but not pain in normal skin in humans. Anesthesiology. 1998 Nov;89(5):1060-7. PMID 9821993
  14. Gilron I, Max MB, Lee G, Booher SL, Sang CN, Chappell AS, Dionne RA. 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. 2000 Sep;68(3):320-7. PMID 11014414
  15. Von Bergen NH, Subieta A, Brennan TJ. Effect of intrathecal non-NMDA EAA receptor antagonist LY293558 in rats: a new class of drugs for spinal anesthesia. Anesthesiology. 2002 Jul;97(1):177-82. PMID 12131120
  16. Sang CN, Ramadan NM, Wallihan RG, Chappell AS, Freitag FG, Smith TR, Silberstein SD, Johnson KW, Phebus LA, Bleakman D, Ornstein PL, Arnold B, Tepper SJ, Vandenhende F. LY293558, a novel AMPA/GluR5 antagonist, is efficacious and well-tolerated in acute migraine. Cephalalgia. 2004 Jul;24(7):596-602. PMID 15196302
  17. Lee HJ, Pogatzki-Zahn EM, Brennan TJ. The effect of the AMPA/kainate receptor antagonist LY293558 in a rat model of postoperative pain. Journal of Pain. 2006 Oct;7(10):768-77. PMID 17018337
  18. Jin HC, Keller AJ, Jung JK, Subieta A, Brennan TJ. Epidural tezampanel, an AMPA/kainate receptor antagonist, produces postoperative analgesia in rats. Anesthesia and Analgesia. 2007 Oct;105(4):1152-9. PMID 17898404
  19. Alt A, Weiss B, Ogden AM, Li X, Gleason SD, Calligaro DO, Bleakman D, Witkin JM. 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 (Berlin). 2006 Apr;185(2):240-7. PMID 16470401

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Tezampanel LY 293 55 likarskij zasib rozroblenij farmacevtichnoyu kompaniyeyu Eli Lilly Mehanizm diyi polyagaye v antagonizmi efektiv AMRA ta kayinatnih receptoriv z bilsh visokoyu afinnistyu do subodinici GluR5 kayinatnogo receptora Preparatu pritamanna ta diya Mehanizm nejroprotektornogo vplivu na CNS polyagaye shonajmenshe chastkovo v blokuvanni transportu kalciyu vseredinu nejroniv Tezampanel Sistematichna nazva IUPAC 3S 4aR 6R 8aR 6 2 1H tetrazol 5 yl ethyl decahydroisoquinoline 3 carboxylic acid Identifikatori Nomer CAS 150131 78 5 Kod ATC PubChem 127894 Himichni dani Formula C13H21N5O2 Mol masa 279 338 g mol SMILES eMolecules amp PubChem Farmakokinetichni dani Biodostupnist Metabolizm Period napivrozpadu Vidilennya Terapevtichni zasterezhennya Kat vagitnosti Dozvolenij dlya naukovih doslidzhen Shlyahi vvedennya Tezampanel maye takozh znachnu kilkist efektiv potencijno pridatnih yak dlya terapevtichnogo vikoristannya tak i dlya vikoristannya v naukovih doslidzhennyah Vin polegshuye abstinentnij sindrom vid morfinu ta inshih opioyidiv a takozh istotno galmuye rozvitok zvikannya do nih Okrim togo tezampanel viyavlyaye antigiperanalgetichni ta analgetichni efekti Okrim togo pri doslidah na tvarinah dana rechovina pokazala anksiolitichni vlastivosti v rezultati chogo bula rekomendovana dlya vikoristannya yak anksiolitik dlya lyudej LiteraturaGilron I LY 293558 Eli Lilly amp Co Current Opinion in Investigational Drugs 2001 Sep 2 9 1273 8 PMID 11717815 Ornstein PL Arnold MB Augenstein NK Lodge D Leander JD Schoepp DD 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 1993 Jul 9 36 14 2046 8 PMID 8393116 Schoepp DD Lodge D Bleakman D Leander JD Tizzano JP Wright RA Palmer AJ Salhoff CR Ornstein PL 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 1995 Sep 34 9 1159 68 PMID 8532186 Bleakman R Schoepp DD Ballyk B Bufton H Sharpe EF Thomas K Ornstein PL Kamboj RK 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 1996 Apr 49 4 581 5 PMID 8609884 Li H Rogawski MA GluR5 kainate receptor mediated synaptic transmission in rat basolateral amygdala in vitro Neuropharmacology 1998Oct Nov 37 10 11 1279 86 PubMed PMID 9849665 Bullock R Graham DI Swanson S McCulloch J Neuroprotective effect of the AMPA receptor antagonist LY 293558 in focal cerebral ischemia in the cat Journal of Cerebral Blood Flow and Metabolism 1994 May 14 3 466 71 PMID 8163588 Rogawski MA Kurzman PS Yamaguchi SI Li H Role of AMPA and GluR5 kainate receptors in the development and expression of amygdala kindling in the mouse Neuropharmacology 2001 40 1 28 35 PubMed PMID 11077068 Liljequist S Cebers G Kalda A 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 1995 Nov 27 50 11 1761 74 PMID 8615854 Rasmussen K Kendrick WT Kogan JH Aghajanian GK A selective AMPA antagonist LY293558 suppresses morphine withdrawal induced activation of locus coeruleus neurons and behavioral signs of morphine withdrawal Neuropsychopharmacology 1996 Nov 15 5 497 505 PMID 8914123 Kest B McLemore G Kao B Inturrisi CE 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 Journal of Pharmacology and Experimental Therapeutics 1997 Dec 283 3 1249 55 PMID 9400000 McLemore GL Kest B Inturrisi CE The effects of LY293558 an AMPA receptor antagonist on acute and chronic morphine dependence Brain Research 1997 Dec 5 778 1 120 6 PMID 9462883 Carlezon WA Jr Rasmussen K Nestler EJ AMPA antagonist LY293558 blocks the development without blocking the expression of behavioral sensitization to morphine Synapse 1999 Mar 15 31 4 256 62 PMID 10051106 Sang CN Hostetter MP Gracely RH Chappell AS Schoepp DD Lee G Whitcup S Caruso R Max MB AMPA kainate antagonist LY293558 reduces capsaicin evoked hyperalgesia but not pain in normal skin in humans Anesthesiology 1998 Nov 89 5 1060 7 PMID 9821993 Gilron I Max MB Lee G Booher SL Sang CN Chappell AS Dionne RA 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 2000 Sep 68 3 320 7 PMID 11014414 Von Bergen NH Subieta A Brennan TJ Effect of intrathecal non NMDA EAA receptor antagonist LY293558 in rats a new class of drugs for spinal anesthesia Anesthesiology 2002 Jul 97 1 177 82 PMID 12131120 Sang CN Ramadan NM Wallihan RG Chappell AS Freitag FG Smith TR Silberstein SD Johnson KW Phebus LA Bleakman D Ornstein PL Arnold B Tepper SJ Vandenhende F LY293558 a novel AMPA GluR5 antagonist is efficacious and well tolerated in acute migraine Cephalalgia 2004 Jul 24 7 596 602 PMID 15196302 Lee HJ Pogatzki Zahn EM Brennan TJ The effect of the AMPA kainate receptor antagonist LY293558 in a rat model of postoperative pain Journal of Pain 2006 Oct 7 10 768 77 PMID 17018337 Jin HC Keller AJ Jung JK Subieta A Brennan TJ Epidural tezampanel an AMPA kainate receptor antagonist produces postoperative analgesia in rats Anesthesia and Analgesia 2007 Oct 105 4 1152 9 PMID 17898404 Alt A Weiss B Ogden AM Li X Gleason SD Calligaro DO Bleakman D Witkin JM 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 Berlin 2006 Apr 185 2 240 7 PMID 16470401

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