Devazepid

Devazepid
IUPAC ime
	N-(1-methyl- 2-oxo- 5-phenyl- 3H-1,4-benzodiazepin-3-yl)- 1H-indole -2-carboxamide
Identifikatori
CAS broj	103420-77-5
ATC kod	none
PubChem	CID 59751
IUPHAR/BPS	878
KEGG	D02693
ChEMBL	CHEMBL153326
Hemijski podaci
Formula	C25H20N4O2
Molarna masa	408.452 g/mol
	SMILES CN1C2=CC=CC=C2C(=NC(C1=O)NC(=O)C3=CC4=CC=CC=C4N3)C5=CC=CC=C5; ;

Devazepid (L-364,718, MK-329) je lek koji je strukturni derivat benzodiazepinske familije, ali se po dejstvu veoma razlikuje od većine benzodiazepina. On nema afiniteta za GABA_A receptore i umesto toga deluje kao holecistokininski antagonist koji je selektivan za CCK_A tip receptora.^[1] On povećava apetit i ubrzava želudačano pražnjenje,^[2]^[3] i smatra se da on potencijalno može da služi kao lek za niz gastrointestinalnih problema, među kojima su dispepsija, gastropareza i gastroezofagealna refluksna bolest.^[4] On je u širokoj upotrebi u naučnim istraživanjima CCK_A receptora.^[5]^[6]^[7]

Reference

^ Hill, D. R.; Woodruff, G. N. (1990-09-03). „Differentiation of central cholecystokinin receptor binding sites using the non-peptide antagonists MK-329 and L-365,260”. Brain Research. 526 (2): 276—83. PMID 2257485. doi:10.1016/0006-8993(90)91232-6.
^ Cooper, S. J.; Dourish, C. T. (децембар 1990). „Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding”. Physiology & Behavior. 48 (6): 849—57. PMID 1982361. doi:10.1016/0031-9384(90)90239-z.
^ Cooper, S. J.; Dourish, C. T.; Clifton, P. G. (1992). „CCK antagonists and CCK-monoamine interactions in the control of satiety”. The American Journal of Clinical Nutrition. 55 (1 Suppl): 291S—295S. PMID 1728842. doi:10.1093/ajcn/55.1.291s.
^ Scarpignato, C.; Varga, G.; Corradi, C. (1993). „Effect of CCK and its antagonists on gastric emptying”. Journal of Physiology, Paris. 87 (5): 291—300. PMID 8298606. doi:10.1016/0928-4257(93)90035-r.
^ Weller, A. (јул 2006). „The ontogeny of postingestive inhibitory stimuli: Examining the role of CCK”. Developmental Psychobiology. 48 (5): 368—79. PMID 16770766. doi:10.1002/dev.20148.
^ Savastano, D. M.; Covasa, M. (2007-10-22). „Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors”. Physiology & Behavior. 92 (3): 434—42. PMID 17531277. doi:10.1016/j.physbeh.2007.04.017.
^ Evans, B. E.; Rittle, K. E.; DiPardo, R. M.; Freidinger, R. M.; Whitter,W. L.; People,W. T.; Lendell, G. F.; Veber, D. F.; Anderson, P. S.; Chang, R. S. L.; Lotti, V. J.; Cerino, D. J.; Chen, T. B.; Kling, P. J.; Kunkel, K. A.; Springer, J. P.; Hirschfield, J. (1988). „Methods for drug discovery: Development of potent, selective, orally effective cholecystokinin antagonists”. J. Med. Chem. 31 (12): 2235—2246. PMID 2848124. doi:10.1021/jm00120a002.

Spoljašnje veze

[1] Hill, D. R.; Woodruff, G. N. (1990-09-03). „Differentiation of central cholecystokinin receptor binding sites using the non-peptide antagonists MK-329 and L-365,260”. Brain Research. 526 (2): 276—83. PMID 2257485. doi:10.1016/0006-8993(90)91232-6.

[2] Cooper, S. J.; Dourish, C. T. (децембар 1990). „Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding”. Physiology & Behavior. 48 (6): 849—57. PMID 1982361. doi:10.1016/0031-9384(90)90239-z.

[3] Cooper, S. J.; Dourish, C. T.; Clifton, P. G. (1992). „CCK antagonists and CCK-monoamine interactions in the control of satiety”. The American Journal of Clinical Nutrition. 55 (1 Suppl): 291S—295S. PMID 1728842. doi:10.1093/ajcn/55.1.291s.

[4] Scarpignato, C.; Varga, G.; Corradi, C. (1993). „Effect of CCK and its antagonists on gastric emptying”. Journal of Physiology, Paris. 87 (5): 291—300. PMID 8298606. doi:10.1016/0928-4257(93)90035-r.

[5] Weller, A. (јул 2006). „The ontogeny of postingestive inhibitory stimuli: Examining the role of CCK”. Developmental Psychobiology. 48 (5): 368—79. PMID 16770766. doi:10.1002/dev.20148.

[6] Savastano, D. M.; Covasa, M. (2007-10-22). „Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors”. Physiology & Behavior. 92 (3): 434—42. PMID 17531277. doi:10.1016/j.physbeh.2007.04.017.

[7] Evans, B. E.; Rittle, K. E.; DiPardo, R. M.; Freidinger, R. M.; Whitter,W. L.; People,W. T.; Lendell, G. F.; Veber, D. F.; Anderson, P. S.; Chang, R. S. L.; Lotti, V. J.; Cerino, D. J.; Chen, T. B.; Kling, P. J.; Kunkel, K. A.; Springer, J. P.; Hirschfield, J. (1988). „Methods for drug discovery: Development of potent, selective, orally effective cholecystokinin antagonists”. J. Med. Chem. 31 (12): 2235—2246. PMID 2848124. doi:10.1021/jm00120a002.

[1]

[2]

[3]

[4]

[5]

[6]

[7]