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N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide

N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide Structure
N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide
  • CAS No.740873-06-7
  • Chemical Name:N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide
  • CBNumber:CB72484704
  • Molecular Formula:C23H38N4O3S
  • Formula Weight:450.64
  • MOL File:740873-06-7.mol
N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide Property
  • Density 1.169
  • storage temp. Store at -20°C
  • solubility Soluble in DMSO
  • form Solid
  • pka 11.49±0.40(Predicted)
  • color White to light yellow
  • FDA UNII LQ54E5B4EW
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements

N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide Chemical Properties,Usage,Production

  • Uses Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
  • in vivo

    In rats Naluzotan shows 11% oral bioavailability with a serum t1/2 of 2?3.5 h when administrated po, attaining a Cmax level of 24 ± 13 ng/mL (3 mg/kg, po). Naluzotan shows significant brain penetration, achieving a brain:serum concentration ratio of approximately 0.5 in the rat at 1 h following either intravenous or oral administration and reaching brain concentration approximately equivalent to that of buspirone. In dogs the pharmacokinetic profile of naluzotan shows 16% oral bioavailability, a serum t1/2 of 1.1 h po, and a Cmax level of 174 ± 141 ng/mL (3 mg/kg, po)[1]. PRX-00023 (0.01-0.05 mg/kg, i.p.) significantly reduces USV rates, but done of these doses produce sedation in rats[2].

  • IC 50 5-HT1A Receptor: 20 nM (IC50); 5-HT1A Receptor: 5.1 nM (Ki); hERG K+ channel: 3800 nM (IC50)
  • References [1] Becker OM, et al. An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. J Med Chem. 2006 Jun 1;49(11):3116-35. DOI:10.1021/jm0508641
    [2] Brunelli SA, et al. PRX-00023, a selective serotonin 1A receptor agonist, reduces ultrasonic vocalizations in infant rats bred for high infantile anxiety. Pharmacol Biochem Behav. 2009 Nov;94(1):8-15. DOI:10.1016/j.pbb.2009.06.014
N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide Preparation Products And Raw materials
Raw materials
Preparation Products
N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide Suppliers
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N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide Spectrum
740873-06-7, N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamideRelated Search:
  • 抑制剂
  • C23H38N4O3S
  • 那鲁佐坦
  • N-[3-[4-[4-[[(环己基甲基)磺酰基]氨基]丁基]-1-哌嗪基]苯基]乙酰胺
  • 化合物 T16265
  • KISS1R激动剂
  • N-[3-[4-[4-[(环己基甲基磺酰基)氨基]丁基]哌嗪-1-基]苯基]乙酰胺
  • 740873-06-7
  • Acetamide, N-[3-[4-[4-[[(cyclohexylmethyl)sulfonyl]amino]butyl]-1-piperazinyl]phenyl]-
  • TAK-448
  • PRX 00023
  • Unii-lq54E5B4ew
  • Naluzotan
  • N-[3-[4-[4-[(Cyclohexylmethylsulfonyl)amino]butyl]piperazin-1-yl]phenyl]acetamide

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