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阿米舒必利

高效的高选择性D 2 / D 3受体拮抗剂

规格或纯度: ≥98%

CAS编号: 71675-85-9
分子式: C₁₇H₂₇N₃O₄S
分子量: 369.48
EC号: 275-831-7
MDL号: MFCD00866691
PubChem编号: 2159

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货号 (SKU)	包装规格	是否现货
A129432-50mg	50mg	现货
A129432-250mg	250mg	现货
A129432-1g	1g	现货
A129432-5g	5g	现货
A129432-25g	25g	现货
A129432-100g	100g	现货

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D2 receptor Antagonist D3 receptor Antagonist

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基本描述

规格或纯度	≥98%
英文名称	Amisulpride
别名	阿米舒必利；4-氨基-N-[(1-乙基-2-吡咯烷基)甲基]-5-乙磺酰基-2-甲氧基苯甲酰胺；氨磺必利
英文别名	4-Amino-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-ethylsulfonyl-2-methoxybenzamide;DAN-2163;Deniban;DAN 2163; DAN2163; Solian;4-amino-N-((1-ethylpyrrolidin-2-yl)methyl)-5-(ethylsulfonyl)-2-methoxybenzamide
生化机理	Amisulpride is a selective, potent D2DR and D3DR inhibitor. (Ki values are 2.8 and 3.2 nM respectively for human D2DR and D3DR and > 1000 nM for human D1DR, D4DR and D5DR.) Amisulpride exhibits selectivity for presynaptic dopamine autoreceptors at low doses and blocks postsynaptic D2DR/D3DR at higher doses. Amisulpride interacts with limbic D2-like receptors .Potent, highly selective D 2 /D 3 receptor antagonist (K i values are 2.8 and 3.2 nM for D 2 and D 3 receptors respectively). Shows atypical antipsychotic effects in vivo . Orally active. Shows limbic selectivity.
储存温度	2-8°C储存
运输条件	冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	A selective D2DR and D3DR inhibitor. A selective D2DR and D3DR inhibitor.

名称和标识符

EC号	275-831-7
IUPAC Name	4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide
INCHI	InChI=1S/C17H27N3O4S/c1-4-20-8-6-7-12(20)11-19-17(21)13-9-16(25(22,23)5-2)14(18)10-15(13)24-3/h9-10,12H,4-8,11,18H2,1-3H3,(H,19,21)
InChi Key	NTJOBXMMWNYJFB-UHFFFAOYSA-N
Canonical SMILES	CCN1CCCC1CNC(=O)C2=CC(=C(C=C2OC)N)S(=O)(=O)CC
分子式	C₁₇H₂₇N₃O₄S
PubChem CID	2159
分子量	369.48

数据库链接

PubChem CID	2159
ChEBI	CHEBI:64045
ChEMBL Ligand	CHEMBL243712
DrugBank Ligand	DB06288
BindingDB Ligand	81790
Wikipedia	Amisulpride
CAS Registry No.	71675-85-9
PEP	amisulpride
Immunopaedia Search	amisulpride
DrugCentral Ligand	179
GPCRdb Ligand	amisulpride

化学和物理性质

溶解性	Soluble in water (partly), dichloromethane, chloroform, DMSO (50 mM), 1eq. HCl (25 mM), methanol, and ethanol (74 mg/ml at 25 °C).
敏感性	对热、湿度和光线敏感
熔点	127 °C

安全信息

象形图	Harmful
信号词	Warning
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation H335: May cause respiratory irritation H302: Harmful if swallowed H312: Harmful in contact with skin H332: Harmful if inhaled
预防措施声明	P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P270,P304+P340,P403+P233,P362+P364,P330,P264+P265,P301+P317,P317,P337+P317,P332+P317,P319
WGK Germany	3
RTECS	CV2308701
Reaxy-Rn	6876191
Merck Index	485
个人防护装备	dust mask type N95 (US), Eyeshields, Gloves

靶标

Target ID

215

名称

D₂ receptor

缩写名

SHP2

家族

Dopamine receptors

别名

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Rat	7	444	8q23	Drd2	dopamine receptor D2
Human	7	443	11q23.2	DRD2	dopamine receptor D2
Mouse	7	444	9 26.72 cM	Drd2	dopamine receptor D2

RefSeq Protein

NP_036679 (Rn) , NP_000786 (Hs) , NP_034207 (Mm)

UniProtKB

P61169 (Rn) , P14416 (Hs) , P61168 (Mm)

OMIM

126450 (Hs)

RefSeq Nucleotide

NM_000795 (Hs) , NM_012547 (Rn) , NM_010077 (Mm)

Entrez Gene

1813 (Hs) , 24318 (Rn) , 13489 (Mm)

Ensembl Gene

ENSG00000149295 (Hs) , ENSMUSG00000032259 (Mm) , ENSRNOG00000008428 (Rn)

Orphanet

121177 (Hs)

Protein GI

6978777 (Rn) , 148747212 (Mm) , 17986270 (Hs)

GPCRdb

drd2_human (Hs) , drd2_mouse (Mm) , drd2_rat (Rn)

UniProtKB ID/Entry name

DRD2_HUMAN (Hs) , DRD2_MOUSE (Mm) , DRD2_RAT (Rn)

DrugBank Target

P14416 (Hs)

ChEMBL Target

CHEMBL217 (Hs) , CHEMBL3427 (Mm) , CHEMBL339 (Rn)

Target ID

216

名称

D₃ receptor

缩写名

SHP2

家族

Dopamine receptors

别名

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Rat	7	446	11q21	Drd3	dopamine receptor D3
Human	7	400	3q13.31	DRD3	dopamine receptor D3
Mouse	7	446	16 28.44 cM	Drd3	dopamine receptor D3

RefSeq Protein

NP_058836 (Rn) , NP_000787 (Hs) , NP_031903 (Mm)

UniProtKB

P19020 (Rn) , P35462 (Hs) , P30728 (Mm)

OMIM

126451 (Hs)

RefSeq Nucleotide

NM_000796 (Hs) , NM_017140 (Rn) , NM_007877 (Mm)

Entrez Gene

1814 (Hs) , 29238 (Rn) , 13490 (Mm)

Ensembl Gene

ENSG00000151577 (Hs) , ENSMUSG00000022705 (Mm) , ENSRNOG00000060806 (Rn)

Orphanet

121179 (Hs)

Protein GI

8393271 (Rn) , 89191863 (Hs) , 6681221 (Mm)

GPCRdb

drd3_human (Hs) , drd3_mouse (Mm) , drd3_rat (Rn)

UniProtKB ID/Entry name

DRD3_HUMAN (Hs) , DRD3_MOUSE (Mm) , DRD3_RAT (Rn)

DrugBank Target

P35462 (Hs)

ChEMBL Target

CHEMBL3441 (Mm) , CHEMBL3138 (Rn) , CHEMBL234 (Hs)

关联配体

Ligand ID	963
名称	amisulpride
别名	(±)-amisulpride
类别	Synthetic organic
学名	4-amino-N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	The approved drug amisulpride is a racemic mixture of (+)-amisulpride and (-)-amisulpride. The structure shown here does not specify stereochemistry and represents the mixture. The links to external resources in the table above all match the INN-assigned compound amisulpride without stereochemistry specified. Alternative stereoisomers are represented by CID 5746246 and CID 3055076. The INN-assigned compound sultopride has a similar but distinct structure to amisulpride; however the nomenclature for these two compounds is sometimes used interchangeably on other resources.