阿米夫胺

**阿米夫胺**
臨床資料
其他名稱	(+)-4-(二甲氨基)-α,2-二甲基苯乙胺
给药途径	口服
ATC碼	未分配;
法律規範狀態
法律規範	不受管制;
识别信息
	IUPAC命名法 4-[(2S)-2-Aminopropyl]-N,N,3-trimethylaniline; ;
CAS号	77518-07-1
PubChem CID	71221;
ChemSpider	64356 ;
UNII	NE25WV9C8S;
ChEMBL	ChEMBL30344 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID00228222 ;
化学信息
化学式	C12H20N2
摩尔质量	192.31 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES N(c1cc(c(cc1)C[C@@H](N)C)C)(C)C;
	InChI InChI=1S/C12H20N2/c1-9-7-12(14(3)4)6-5-11(9)8-10(2)13/h5-7,10H,8,13H2,1-4H3/t10-/m0/s1 ; Key:HFQMYSHATTXRTC-JTQLQIEISA-N ;

阿米夫胺（INN：amiflamine；开发代号：FLA-336）是单胺氧化酶A（英语：Monoamine oxidase A）的可逆抑制剂，对氨基脲敏感性胺氧化酶（英语：Primary-amine oxidase）（SSAO）也有一定抑制作用，并且是血清素释放剂（英语：Serotonin releasing agent）。^[1]^[2]^[3]^[4]它是苯乙胺和安非他明的衍生物。^[1]该化合物的(+)-对映体是活性立体异构体。^[2]

相对于去甲肾上腺素能和多巴胺能神经元，阿米夫胺优先抑制血清素能神经元中的单胺氧化酶A（英语：Monoamine oxidase A）。^[5]^[6]换句话说，在低剂量时，它可用于选择性抑制血清素细胞中的单胺氧化酶A，而在较高剂量时，它会失去选择性。^[5]^[6]这一特性归因于阿米夫胺对血清素转运蛋白的亲和力高于去甲肾上腺素和多巴胺转运蛋白，因为转运蛋白介导的运输是阿米夫胺进入单胺能神经元的必要条件。^[6]

参见[编辑]

单胺氧化酶抑制剂

参考资料[编辑]

^ ^1.0 ^1.1 Ask AL, Högberg K, Schmidt L, Kiessling H, Ross SB. (+)-4-Dimethylamino-2,alpha-dimethylphenethylamine (FLA 336(+)), a selective inhibitor of the A form of monoamine oxidase in the rat brain. Biochemical Pharmacology. April 1982, 31 (7): 1401–6. PMID 7092929. doi:10.1016/0006-2952(82)90035-1.
^ ^2.0 ^2.1 Fowler CJ, Eriksson M, Thorell G, Magnusson O. Stereoselective inhibition of monoamine oxidase and semicarbazide-sensitive amine oxidase by 4-dimethylamino-2,alpha-dimethylphenethylamine (FLA 336). Naunyn-Schmiedeberg's Archives of Pharmacology. October 1984, 327 (4): 279–84. PMID 6514012. S2CID 25342831. doi:10.1007/bf00506237.
^ Morikawa F, Ueda T, Arai Y, Kinemuchi H. Inhibition of monoamine oxidase A-form and semicarbazide-sensitive amine oxidase by selective and reversible monoamine oxidase-A inhibitors, amiflamine and FLA 788(+). Pharmacology. 1986, 32 (1): 38–45. PMID 3945672. doi:10.1159/000138150.
^ Ask AL, Fagervall I, Huang RB, Ross SB. Release of 3H-5-hydroxytryptamine by amiflamine and related phenylalkylamines from rat occipital cortex slices. Naunyn-Schmiedeberg's Archives of Pharmacology. June 1989, 339 (6): 684–9. PMID 2770890. S2CID 21817180. doi:10.1007/bf00168662.
^ ^5.0 ^5.1 Fowler CJ, Magnusson O, Ross SB. Intra- and extraneuronal monoamine oxidase. Blood Vessels. 1984, 21 (3): 126–31. PMID 6202347. doi:10.1159/000158505.
^ ^6.0 ^6.1 ^6.2 Ask AL, Fagervall I, Ross SB. Selective inhibition of monoamine oxidase in monoaminergic neurons in the rat brain. Naunyn-Schmiedeberg's Archives of Pharmacology. September 1983, 324 (2): 79–87. PMID 6646243. S2CID 403633. doi:10.1007/BF00497011.

[pmid7092929-1] 1.0 ^1.1 Ask AL, Högberg K, Schmidt L, Kiessling H, Ross SB. (+)-4-Dimethylamino-2,alpha-dimethylphenethylamine (FLA 336(+)), a selective inhibitor of the A form of monoamine oxidase in the rat brain. Biochemical Pharmacology. April 1982, 31 (7): 1401–6. PMID 7092929. doi:10.1016/0006-2952(82)90035-1.

[pmid6514012-2] 2.0 ^2.1 Fowler CJ, Eriksson M, Thorell G, Magnusson O. Stereoselective inhibition of monoamine oxidase and semicarbazide-sensitive amine oxidase by 4-dimethylamino-2,alpha-dimethylphenethylamine (FLA 336). Naunyn-Schmiedeberg's Archives of Pharmacology. October 1984, 327 (4): 279–84. PMID 6514012. S2CID 25342831. doi:10.1007/bf00506237.

[pmid3945672-3] Morikawa F, Ueda T, Arai Y, Kinemuchi H. Inhibition of monoamine oxidase A-form and semicarbazide-sensitive amine oxidase by selective and reversible monoamine oxidase-A inhibitors, amiflamine and FLA 788(+). Pharmacology. 1986, 32 (1): 38–45. PMID 3945672. doi:10.1159/000138150.

[pmid2770890-4] Ask AL, Fagervall I, Huang RB, Ross SB. Release of 3H-5-hydroxytryptamine by amiflamine and related phenylalkylamines from rat occipital cortex slices. Naunyn-Schmiedeberg's Archives of Pharmacology. June 1989, 339 (6): 684–9. PMID 2770890. S2CID 21817180. doi:10.1007/bf00168662.

[pmid6202347-5] 5.0 ^5.1 Fowler CJ, Magnusson O, Ross SB. Intra- and extraneuronal monoamine oxidase. Blood Vessels. 1984, 21 (3): 126–31. PMID 6202347. doi:10.1159/000158505.

[pmid6646243-6] 6.0 ^6.1 ^6.2 Ask AL, Fagervall I, Ross SB. Selective inhibition of monoamine oxidase in monoaminergic neurons in the rat brain. Naunyn-Schmiedeberg's Archives of Pharmacology. September 1983, 324 (2): 79–87. PMID 6646243. S2CID 403633. doi:10.1007/BF00497011.

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