所有图片(1)
别名:
(–)-喹吡罗 单盐酸盐, 反式 -(-) (4aR)-4,4a,5,6,7,8,8a,9-八氢-5-丙基-1H-吡唑并 [3,4-g] 喹啉 单盐酸盐, LY-171,555
经验公式（希尔记法）:
C13H21N3 · HCl
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质量水平
检测方案
≥98% (HPLC)
形式
solid
旋光性
[α]25/D −124.5°, c = 0.4 in H2O(lit.)
储存条件
desiccated
颜色
white
溶解性
0.1 M HCl: 23 mg/mL
H2O: 7.3 mg/mL
储存温度
−20°C
SMILES字符串
Cl.[H][C@]12CCCN(CCC)[C@]1([H])Cc3c[nH]nc3C2
InChI
1S/C13H21N3.ClH/c1-2-5-16-6-3-4-10-7-12-11(8-13(10)16)9-14-15-12;/h9-10,13H,2-8H2,1H3,(H,14,15);1H/t10-,13-;/m1./s1
InChI key
HJHVRVJTYPKTHX-HTMVYDOJSA-N
基因信息
human ... DRD2(1813) , DRD3(1814)
应用
(-)-喹吡罗盐酸盐在各种实验中作为选择性D2多巴胺（DA）受体激动剂。
生化/生理作用
喹吡罗是多巴胺激动剂，对D2 和D3多巴胺受体亚型具有高亲和力。大鼠脑中与特异性[3H]喹吡罗结合是可饱和的，具体结合情况取决于温度、膜浓度、钠浓度和鸟嘌呤核苷酸等因素。 推定D2 多巴胺受体激动剂喹吡罗（LY 171,555）是体内和体外研究中使用最广的D2激动剂。盐酸喹吡罗是(±)-喹吡罗的活性对映异构体。饱和分析显示，其具有高亲和力结合的特征（KD = 2.3 +/- 0.3 nM），可通过缔合-解离动力学得到证实。[3H]喹吡罗结合位点的区域分布与[3H]螺环哌啶酮结合位点的分布大致平行，在纹状体、伏隔核和嗅结节中密度最大。许多药物，主要是单胺氧化酶抑制剂（MAOl），抑制[3H]喹吡罗的结合，但不抑制[3H]螺环哌啶酮或[3H]（-）N-n-丙基去甲阿朴吗啡的结合。在大鼠大鼠纹状体膜中，这一作用似乎由不涉及MAO酶活性的机制产生。临床上用于抗抑郁的 MAOI 显示出在[3H]喹吡罗标记和[3H]螺环哌啶酮标记的位点间具有选择性，一些结构相关的炔丙基胺、N-乙酰基乙二胺衍生物和其他药物（如异喹胍和苯基双胍）也是如此。MAOI 中的氯吉兰和 Ro 41-1049最为有效。MAOI 与新结合位点相互作用，这一位点由[3H]喹吡罗标记或调节[3H]喹吡罗结合。此位点可能与D2样多巴胺受体有关。
法律信息
经美国礼来公司（Eli Lilly and Company）许可生产和销售。
WGK
WGK 3
个人防护装备
Eyeshields, Gloves, type N95 (US)
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