Afloqualone；氟喹酮
货号：
IA2100
品牌：
Jinpan
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产品简介
| MDL | MFCD00867693 |
| EC | EINECS 1592732-453-0 |
| InChIKey | VDOSWXIDETXFET-UHFFFAOYSA-N |
| InChI | InChI=1S/C16H14FN3O/c1-10-4-2-3-5-14(10)20-15(9-17)19-13-7-6-11(18)8-12(13)16(20)21/h2-8H,9,18H2,1H3 |
| PubChem CID | 2040 |
| 别名 | Aroft;HQ495;Afloqualon |
| 英文名称 | Afloqualone |
| CAS | 56287-74-2 |
| 分子式 | C16H14FN3O |
| 分子量 | 283.3 |
| 纯度 | HPLC≥98% |
| 单位 | 瓶 |
| 生物活性 | Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the GABAα receptor. Afloqualone has antivertiginous and sedative effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site[1]. |
| In Vivo | Effects of afloqualone on mono- (MSR) and poly-synaptic reflex (PSR) potentials and alpha- and gamma-rigidities were studied in experimental animals. Afloqualone dose dependently inhibited both MSR and PSR potentials in spinalized cats.Afloqualone, like other well known centrally acting muscle relaxants except for baclofen, more strongly inhibits the polysynaptic pathway than the mono-synaptic pathway of the spinal cord as well as more strongly the gamma-system than the alpha-system.[1] |
| SMILES | O=C1N(C2=CC=CC=C2C)C(CF)=NC3=C1C=C(N)C=C3 |
| 靶点 | GABA Receptor |
| 细胞实验 | In rats and cats, afloqualone dose dependently relaxed both alpha- and gamma-rigidity when administered p.o. as well as i.v. Its 50% inhibitory dose for alpha-rigidity was 1.5-2 times larger than that for gamma-rigidity. Tolperisone also relaxed both rigidities in i.v. administration, but had little effect when given p.o. Only mephenesin relaxed the post-ischaemic spinal rigidity in cats. [1] |
| 数据来源文献 | [1]. T Ochiai, et al. Pharmacological studies on 6-amino-2-fluoromethyl-3-(O-tolyl)-4(3H)-quinazolinone (afloqualone), a new centrally acting muscle relaxant. (II) Effects on the spinal reflex potential and the rigidity. Jpn J Pharmacol. 1982 Jun;32(3):427-38. |
| 规格 | 100mg |
Afloqualone是一种GABA-A受体β亚型激动剂。