デバゼピド

デバゼピド
IUPAC命名法による物質名
	IUPAC名 N-(1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl)-1H-indole-2-carboxamide;
データベースID
CAS番号;	103420-77-5
ATCコード	none
PubChem	CID: 443375
IUPHAR/BPS（英語版）	878
ChemSpider	391607
UNII	JE6P7QY7NH
KEGG	D02693
ChEMBL	CHEMBL9506
化学的データ
化学式	C25H20N4O2
分子量	408.46 g·mol−1
	SMILES O=C(c2cc1ccccc1[nH]2)N[C@H]3/N=C(\c4ccccc4N(C3=O)C)c5ccccc5;
	InChI InChI=1S/C25H20N4O2/c1-29-21-14-8-6-12-18(21)22(16-9-3-2-4-10-16)27-23(25(29)31)28-24(30)20-15-17-11-5-7-13-19(17)26-20/h2-15,23,26H,1H3,(H,28,30)/t23-/m1/s1 ; Key:NFHRQQKPEBFUJK-HSZRJFAPSA-N ;
	テンプレートを表示

デバゼピド（英：Devazepide^[1]、L-364,718、MK-329）はベンゾジアゼピン系薬物であるが、GABA_A受容体に対する親和性を欠き、代わりにCCK_A受容体拮抗薬として作用するなど、多くのベンゾジアゼピン系薬物とは全く異なる作用を持つ^[2]。食欲を増進させ、胃排出を促進し^[3]^[4]、消化不良、胃不全麻痺、胃食道逆流症を含む様々な胃腸障害の治療薬としての可能性が示唆されている^[5]。また、CCK_A受容体の科学的研究にも広く使われている^[6]^[7]。合成

デバゼピドは他のベンゾジアゼピンと同様の方法で合成される^[8]^[9]。

脚注

^ US 4820834, Evans, Ben E.; Roger M. Freidinger & Mark G. Bock, "Benzodiazepine analogs", published 1989-04-11, assigned to Merck & Co. Inc.
^ “Differentiation of central cholecystokinin receptor binding sites using the non-peptide antagonists MK-329 and L-365,260”. Brain Research 526 (2): 276–83. (September 1990). doi:10.1016/0006-8993(90)91232-6. PMID 2257485.
^ “Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding”. Physiology & Behavior 48 (6): 849–57. (December 1990). doi:10.1016/0031-9384(90)90239-z. PMID 1982361.
^ “CCK antagonists and CCK-monoamine interactions in the control of satiety”. The American Journal of Clinical Nutrition 55 (1 Suppl): 291S–295S. (January 1992). doi:10.1093/ajcn/55.1.291s. PMID 1728842.
^ “Effect of CCK and its antagonists on gastric emptying”. Journal of Physiology, Paris 87 (5): 291–300. (1993). doi:10.1016/0928-4257(93)90035-r. PMID 8298606.
^ “The ontogeny of postingestive inhibitory stimuli: examining the role of CCK”. Developmental Psychobiology 48 (5): 368–79. (July 2006). doi:10.1002/dev.20148. PMID 16770766.
^ “Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors”. Physiology & Behavior 92 (3): 434–42. (October 2007). doi:10.1016/j.physbeh.2007.04.017. PMID 17531277.
^ “Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists”. Journal of Medicinal Chemistry 31 (12): 2235–46. (December 1988). doi:10.1021/jm00120a002. PMID 2848124.
^ EP 1492540, Jackson, Karen, "The use of devazepide as analgesic agent", published 2005-01-05, assigned to ML Laboratories plc

[1] US 4820834, Evans, Ben E.; Roger M. Freidinger & Mark G. Bock, "Benzodiazepine analogs", published 1989-04-11, assigned to Merck & Co. Inc.

[2] “Differentiation of central cholecystokinin receptor binding sites using the non-peptide antagonists MK-329 and L-365,260”. Brain Research 526 (2): 276–83. (September 1990). doi:10.1016/0006-8993(90)91232-6. PMID 2257485.

[3] “Multiple cholecystokinin (CCK) receptors and CCK-monoamine interactions are instrumental in the control of feeding”. Physiology & Behavior 48 (6): 849–57. (December 1990). doi:10.1016/0031-9384(90)90239-z. PMID 1982361.

[4] “CCK antagonists and CCK-monoamine interactions in the control of satiety”. The American Journal of Clinical Nutrition 55 (1 Suppl): 291S–295S. (January 1992). doi:10.1093/ajcn/55.1.291s. PMID 1728842.

[5] “Effect of CCK and its antagonists on gastric emptying”. Journal of Physiology, Paris 87 (5): 291–300. (1993). doi:10.1016/0928-4257(93)90035-r. PMID 8298606.

[6] “The ontogeny of postingestive inhibitory stimuli: examining the role of CCK”. Developmental Psychobiology 48 (5): 368–79. (July 2006). doi:10.1002/dev.20148. PMID 16770766.

[7] “Intestinal nutrients elicit satiation through concomitant activation of CCK(1) and 5-HT(3) receptors”. Physiology & Behavior 92 (3): 434–42. (October 2007). doi:10.1016/j.physbeh.2007.04.017. PMID 17531277.

[8] “Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists”. Journal of Medicinal Chemistry 31 (12): 2235–46. (December 1988). doi:10.1021/jm00120a002. PMID 2848124.

[9] EP 1492540, Jackson, Karen, "The use of devazepide as analgesic agent", published 2005-01-05, assigned to ML Laboratories plc

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デバゼピド

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脚注

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