Eglumegad

Eglumegad
IUPAC ime
	(1S,2S,5R,6S)-2-aminobiciklo[3.1.0]heksan-2,6-dikarboksilna kiselina
Identifikatori
CAS broj	176199-48-7
ATC kod	none
PubChem	CID 213056
IUPHAR/BPS	1396
UNII	ONU5A67T2S
Hemijski podaci
Formula	C8H11NO4
Molarna masa	185,18 g/mol

Eglumegad (LY354740) je lek koji se istražuje za potencijalnu primenu u treatmanu anksioznosti^[1] i zavisnosti.^[2] On je jedinjenje izvedeno iz glutamata. Njegov način dejstva sugeriše mogući novi mehanizam.^[3]

Mehanizam akcije

Eglumegad deluje kao agonist koji je selektivan za grupu II metabotropnih glutamatnih receptora (mGluR₂_/₃).^[4]^[5] Nalazi o direktnoj interakciji sa dopaminskim D2 receptorima su inkonzistentni.^[6]^[7]

Reference

^ Pilc A. LY-354740 (Eli Lilly). Pilc, A. (јануар 2003). „LY-354740 (Eli Lilly)”. IDrugs. 6 (1): 66—71. PMID 12789623.
^ Kłodzińska A, Chojnacka-Wójcik E, Pałucha A, Brański P, Popik P, Pilc A. Kłodzińska, A.; Chojnacka-Wójcik, E.; Pałucha, A.; Brański, P.; Popik, P.; Pilc, A. (децембар 1999). „Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models”. Neuropharmacology. 38 (12): 1831—9. PMID 10608278. doi:10.1016/S0028-3908(99)00066-0.
^ Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD. Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740). Monn, J. A.; Valli, M. J.; Massey, S. M.; Wright, R. A.; Salhoff, C. R.; Johnson, B. G.; Howe, T.; Alt, C. A.; Rhodes, G. A.; Robey, R. L.; Griffey, K. R.; Tizzano, J. P.; Kallman, M. J.; Helton, D. R.; Schoepp, D. D. (фебруар 1997). „a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties”. Journal of Medicinal Chemistry. 40 (4): 528—37. PMID 9046344. doi:10.1021/jm9606756.
^ Schoepp DD, Johnson BG, Wright RA, Salhoff CR, Mayne NG, Wu S, Cockerman SL, Burnett JP, Belegaje R, Bleakman D, Monn JA. Schoepp, D. D.; Johnson, B. G.; Wright, R. A.; Salhoff, C. R.; Mayne, N. G.; Wu, S.; Cockerman, S. L.; Burnett, J. P.; Belegaje, R.; Bleakman, D.; Monn, J. A. (јануар 1997). „LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors”. Neuropharmacology. 36 (1): 1—11. PMID 9144636. doi:10.1016/S0028-3908(96)00160-8.
^ Bond A, Monn JA, Lodge D. Bond, A.; Monn, J. A.; Lodge, D. (април 1997). „A novel orally active group 2 metabotropic glutamate receptor agonist LY354740”. NeuroReport. 8 (6): 1463—6. PMID 9172154. doi:10.1097/00001756-199704140-00027.
^ Seeman P, Caruso C, Lasaga M (2008). „Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268”. Synapse. 62 (2): 154—8. PMID 18000815. doi:10.1002/syn.20482. hdl:11336/108389.
^ Fell, M. J.; Perry, K. W.; Falcone, J. F.; et al. (2009). „In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268)”. J. Pharmacol. Exp. Ther. 331 (3): 1126—36. PMID 19755662. doi:10.1124/jpet.109.160598.

Spoljašnje veze

[1] Pilc A. LY-354740 (Eli Lilly). Pilc, A. (јануар 2003). „LY-354740 (Eli Lilly)”. IDrugs. 6 (1): 66—71. PMID 12789623.

[2] Kłodzińska A, Chojnacka-Wójcik E, Pałucha A, Brański P, Popik P, Pilc A. Kłodzińska, A.; Chojnacka-Wójcik, E.; Pałucha, A.; Brański, P.; Popik, P.; Pilc, A. (децембар 1999). „Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models”. Neuropharmacology. 38 (12): 1831—9. PMID 10608278. doi:10.1016/S0028-3908(99)00066-0.

[3] Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD. Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740). Monn, J. A.; Valli, M. J.; Massey, S. M.; Wright, R. A.; Salhoff, C. R.; Johnson, B. G.; Howe, T.; Alt, C. A.; Rhodes, G. A.; Robey, R. L.; Griffey, K. R.; Tizzano, J. P.; Kallman, M. J.; Helton, D. R.; Schoepp, D. D. (фебруар 1997). „a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties”. Journal of Medicinal Chemistry. 40 (4): 528—37. PMID 9046344. doi:10.1021/jm9606756.

[4] Schoepp DD, Johnson BG, Wright RA, Salhoff CR, Mayne NG, Wu S, Cockerman SL, Burnett JP, Belegaje R, Bleakman D, Monn JA. Schoepp, D. D.; Johnson, B. G.; Wright, R. A.; Salhoff, C. R.; Mayne, N. G.; Wu, S.; Cockerman, S. L.; Burnett, J. P.; Belegaje, R.; Bleakman, D.; Monn, J. A. (јануар 1997). „LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors”. Neuropharmacology. 36 (1): 1—11. PMID 9144636. doi:10.1016/S0028-3908(96)00160-8.

[5] Bond A, Monn JA, Lodge D. Bond, A.; Monn, J. A.; Lodge, D. (април 1997). „A novel orally active group 2 metabotropic glutamate receptor agonist LY354740”. NeuroReport. 8 (6): 1463—6. PMID 9172154. doi:10.1097/00001756-199704140-00027.

[6] Seeman P, Caruso C, Lasaga M (2008). „Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268”. Synapse. 62 (2): 154—8. PMID 18000815. doi:10.1002/syn.20482. hdl:11336/108389.

[7] Fell, M. J.; Perry, K. W.; Falcone, J. F.; et al. (2009). „In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268)”. J. Pharmacol. Exp. Ther. 331 (3): 1126—36. PMID 19755662. doi:10.1124/jpet.109.160598.

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