首页 > 化工企业 > MedChemexpress > (-)-(S)-N-(alpha-乙基苄基)-3-羟基-2-苯基喹啉-4-羧酰胺
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货号: HY-14552

(-)-(S)-N-(alpha-乙基苄基)-3-羟基-2-苯基喹啉-4-羧酰胺

  • 174636-32-9
  • C25H22N2O2
  • 98%
  • 7日

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信息更新时间:2018.06.10
  • (-)-(S)-N-(alpha-乙基苄基)-3-羟基-2-苯基喹啉-4-羧酰胺
  • 98%
  • 10mg
  • 1 mg
  • 7日
  • HY-14552
化合物信息 [查看化合物百科]
化合物英文学名 3-hydroxy-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide 化合物中文学名 (-)-(S)-N-(alpha-乙基苄基)-3-羟基-2-苯基喹啉-4-羧酰胺
CAS号 174636-32-9 分子式 C25H22N2O2
分子量 382.454 精确质量 382.168
LogP 6.0633 PSA 65.71
折射率 1.657 蒸汽压 4.51E-14mmHg at 25°C
密度 1.212g/cm3 沸点 580.4ºC at 760mmHg
闪点 304.8ºC
详细描述
产品描述:Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist (ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM. IC50 Value: 1.4 nM (hNK-3-CHO binding Ki) [1] Target: NK3 receptor in vitro: In vitro studies demonstrated that 53 is a potent functional antagonist of the hNK-3 receptor (reversal of senktide-induced contractions in rabbit isolated iris sphincter muscles and reversal of NKB-induced Ca2+ mobilization in CHO cells stably expressing the hNK-3 receptor), while in vivo this compound showed oral and intravenous activity in NK-3 receptor-driven models (senktide-induced behavioral responses in mice and senktide-induced miosis in rabbits) [1]. Talnetant has high affinity for recombinant human NK3 receptors (pKi 8.7) and demonstrates selectivity over other neurokinin receptors (pKi NK2 = 6.6 and NK1<4). In native tissue-binding studies, talnetant displayed high affinity for the guinea pig NK3 receptor (pKi 8.5) [3]. in vivo: Rectal barostat tests were performed on 102 healthy volunteers, randomized to receive either oral talnetant 25 or 100 mg or placebo over 14-17 days [2]. Talnetant (3-30 mg/kg i.p.) significantly attenuated senktide-induced \'wet dog shake\' behaviors in the guinea pig in a dose-dependent manner. Microdialysis studies demonstrated that acute administration of talnetant (30 mg/kg i.p.) produced significant increases in extracellular dopamine and norepinephrine in the medial prefrontal cortex and attenuated haloperidol-induced increases in nucleus accumbens dopamine levels in the freely moving guinea pigs [3]. Toxicity: Talnetant had no effect on rectal compliance, sensory thresholds or intensity ratings compared with placebo [2]. Clinical trial: Study Of Talnetant Versus Placebo And Risperidone In Schizophrenia. Phase 2
产品链接:http://www.medchemexpress.com/SR1078.html
产品链接:http://www.medchemexpress.cn/talnetant.html

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(-)-(S)-N-(alpha-乙基苄基)-3-羟基-2-苯基喹啉-4-羧酰胺

174636-32-9

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