151227-08-6
- CAS号:151227-08-6
- 英文名:AP521
- 中文名:151227-08-6
- CBNumber:CB74796632
- 分子式:C20H19ClN2O3S
- 分子量:402.89
- MOL File:151227-08-6.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
151227-08-6性质、用途与生产工艺
- 生物活性 AP521 是一个人 5-HT1A 受体激动剂,其 IC50 值为 94 nM。
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靶点
5-HT 1A Receptor
94 nM (IC 50 , in human)
5-HT 1A Receptor
135 nM (IC 50 , in rat)
5-HT 1B Receptor
254 nM (IC 50 , in rat)
5-HT 1B Receptor
5530 nM (IC 50 , in human)
5-HT 1D Receptor
418 nM (IC 50 , in human)
5-HT 5A Receptor
422 nM (IC 50 , in human)
5-HT 7 Receptor
198 nM (IC 50 , in rat)
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体外研究
AP521 is an agonist of human 5-HT 1A receptor with IC 50 s of 135, 94, 254, 5530, 418, 422 and 198 nM for 5-HT 1A (rat), 5-HT 1A (human), 5-HT 1B (rat), 5-HT 1B (human), 5-HT 1D (human), 5-HT 5a (human) and 5-HT 7 (rat), respectively. AP521 also decreases the forskolin-induced cAMP accumulation from 10 nM to 10 μM.
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体内研究
AP521 significantly increases the number of shock acceptances [F(5,105)=4.46, P<0.01] at doses between 0.5 to 10 mg/kg. Oral administration of AP521 at 3 and 10 mg/kg significantly decreases freezing time [F(3,60)=2.89, P<0.05]. AP521 significantly increases the time spent on the open arms by approximately 2-fold as compare to the vehicle treated group [F(3, 36)=4.21, P<0.05 for AP521]. The anxiolytic-like effect of AP521 appears to be dose-related. AP521 significantly increases the extracellular 5-HT level of the medial prefrontal cortex (mPFC) at 10 mg/kg from 0.5 to 1 h after administration. AP521 at 3 mg/kg tends to increase the extracellular 5-HT level, however, this increase is not significant.
- 更新日期:2024/01/25
- 产品编号:HY-100166
- 产品名称:151227-08-6 AP521
- CAS编号:151227-08-6
- 包装:5 mg
- 价格:1700元
- 更新日期:2024/01/25
- 产品编号:HY-100166
- 产品名称:AP521
- CAS编号:
- 包装:10 mg
- 价格:3000元
- 公司名称:范德(北京)生物科技有限责任公司
- 联系电话: 15911056312
- 电子邮件:liming@bio-fount.com
- 国家:中国
- 产品数:9730
- 优势度:58
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:成都超九八生物科技有限公司
- 联系电话:13348960310 13348960310
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- 国家:中国
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- 公司名称:天津普西唐生物医药科技有限公司
- 联系电话:010-60605840 15801484223
- 电子邮件:psaitong@jm-bio.com
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- 公司名称:TargetMol中国(陶术生物)
- 联系电话: 4008200310
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- 联系电话: 1173954148q
- 电子邮件:meishipharma@126.com
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- 优势度:58