a neuronal nicotinic AChR antagonist. Potent ganglioblocker. Hypotensive. Good penetration of biological membranes. Sedative. Secondary analog of Pempidone. Antioxidant, radical scavenger.

Piperidine derivative, C₉H₁₇NO .HCl, synthetic.

• Molecular Weight : 191.70 Da.
  
  
• Melting Point : 195-196 °C.
  
  
• Solubility in : water, ethanol.
  
  
• Purity min. : min. 99.5%.
  TLC (Silufol UV-254, MeOH:NH3(25%) Rf 0.41, development with Dragendorff¨ reagent); NMR (D2O).
  
  
• Physical Form : colorless crystal powder.
  
  
• Chemical Name : 2,2,6,6-tetramethylpiperidone-4 hydrochloride.
  
  
• Biological Activity : For comparative information see the attached tables.
  
  Cell permeant central nicotinic cholinoreceptor blocker without action on skeleton muscle innervation. Nicotinic AChR antagonist, autonomic ganglioblocker [1-3].
  
  Hypotensive (purely anti-nicotinic) without smooth muscles relaxation - up to 80 µg/kg has no antagonism with BaCl2, conc. KCl, noradrenaline, histamine, 5-HT, angiotensin, bradyquinine [4].
  
  Antioxydant [5]: precursor of stable TEMPO nitroxyl radical. Inhibits cell in metastase :
  COLCHICINE-like action [6]:
  Hepatoma 22 (C 3H mice) : 90-270: 35-50: 66-100
  Erlich carcinoma (albino mice): 100-380: 40-85: 66-100
  Brown-Pearce carcinoma (rabbits):15-150: remarkable reduction of metastases and primary tumor.
  
  Sedative, hypnotic [2].
  
  
• Toxicity (LD₅₀) : mice (orally): 200-230 mg/kg - mice (i.v.): 860-950 mg/kg;
  rats (i.v.): 600-700 mg/kg. - mice (i.p.): 350-400 mg/kg;
  rats (i.p.): 600-700 mg/kg - mice (i.m.): 500 mg/kg
  
  
• Storage recommendations : store at room temperature. Solution for use: dissolve in water: 10-³M (2 mg in 10.43 ml), stable for 1-2 days at 20°C.
  
  
• CAS Reg. No. : 33973-59-0 (base), 826-36-8 (HCl), 29334-13-2 (tosilate).
  
  
• Bibliography :
  
  1. Brehteric et al., Nature (1959). 184:1707-1709
  2. Chodera A. et al., Pharm. Zentralhalle (1964). 103(1):17-23
  3. Rojas R.L., Rev. Cubana Farm. (1979). 13:37-45 and 163-173
  4. Rojas R.L., Rev. Cubana Farm. (1979). 16:146-156
  5. Komarov P.G. et al., Dokl. Akad. Nauk SSSR (1987). 297(3):734-737
  6. Brito et al., Rev. Cubana Farm. (1982). 16(2):146-156