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Product details

名称

GSK163090, 羟色胺转运体拮抗剂

分子类型

小分子

英文别名

GSK 163090 | Q27268983 | 1-[3-[2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl]phenyl]-2-imidazolidinone | AKOS030526918 | SCHEMBL2881345 | AC-33679 | 7XI927X82B | HY-14348 | 1-(3-(2-(4-(2-Methyl-5-quinolinyl)-1-piperazinyl)ethyl)phenyl)-2-imidazolidinon

英文名称

GSK163090

货号

G650117-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

GSK163090 is a potent, selective and orally active 5-HT 1A/1B/1D receptor antagonist with pK i values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pK i value of 6.1. GSK163090 has antidepressant and anxiolytic activities In Vitro GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC 50 =6.9). At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED 50 values ranging from 0.03 to 1 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:5-HT 1A Receptor 9.4 (pKi) 5-HT 1B Receptor 8.5 (pKi) 5-HT 1D Receptor 9.7 (pKi) D 2 Receptor 6.3 (pKi) D 3 Receptor 6.7 (pKi) 5-HT 2A Receptor 6 (pKi) 5-HT 2B Receptor 6.3 (pKi) 5-HT 2C Receptor 5.8 (pKi) Human 5-HT 6 Receptor

生化机理

GSK163090 是一种强效、选择性和口服活性 5-HT 1A/1B/1D 受体拮抗剂，pK i 值分别为 9.4/8.5/9.7。GSK163090 可抑制血清素再摄取转运体（SerT）的功能活性，pK i 值为 6.1。GSK163090 具有

CAS号

844903-58-8

分子式

C25H29N5O

分子量

415.53 g/mol

EC号

629-856-9

PubChem编号

11292933

Isomeric SMILES

CC1=NC2=C(C=C1)C(=CC=C2)N3CCN(CC3)CCC4=CC(=CC=C4)N5CCNC5=O

IIUPAC Name

1-[3-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]phenyl]imidazolidin-2-one

INCHI

1S/C25H29N5O/c1-19-8-9-22-23(27-19)6-3-7-24(22)29-16-14-28(15-17-29)12-10-20-4-2-5-21(18-20)30-13-11-26-25(30)31/h2-9,18H,10-17H2,1H3,(H,26,31)

InChi Key

ANGUXJDGJCHGOG-UHFFFAOYSA-N

Smiles

CC1=NC2=C(C=C1)C(=CC=C2)N3CCN(CC3)CCC4=CC(=CC=C4)N5CCNC5=O

PubChem CID

11292933

关联CAS

844903-58-8

MeSH Entry Terms

1-(3-(2-(4-(2-methyl-5-quinolinyl)-1-piperazinyl)ethyl)phenyl)-2-imidazolidinone;GSK163090

溶解性

DMSO : 14.29 mg/mL (34.39 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

415.237 Da

单同位素质量Monoisotopic Mass

415.237 Da

拓扑极表面积Topological Polar Surface Area

51.700 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

607.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.400

ALogP

3.4

作用类型

拮抗剂

作用机制

羟色胺转运体拮抗剂

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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