a neuronal nicotinic AChR antagonist. Potent ganglioblocker. Antihypertensive. Good penetration of biological membranes. Monocyclic analog of TEMECHINE.

Piperidine derivative, C₁₀H₂₁N .C₄H₆O₆, synthetic.

• Molecular Weight : 305.37 Da.
  
  
• Melting Point : 150-151°C
  
  
• Solubility in : water, ethanol.
  
  
• Purity min. : min. 98%.
  TLC (Silufol UV-254, MeOH:NH3(25%) Rf 0.78, development with Dragendorff¨ reagent); NMR (D2O).
  
  
• Physical Form : colorless crystal powder
  
  
• Chemical Name : 1,2,2,6,6-pentamethylpiperidine d-tartrate.
  
  
• Biological Activity : For comparative information see the attached tables. Cell permeant central nicotinic acetylcholine receptor blocker without action on skeleton muscle innervation.
  
  Produces a slowly developing voltage-dependent block of ionoforetically activated cholinergic currents of the lobster gastric mill [3, 4].
  
  CNS activity: see the attached table.
  
  35 mg/kg increases ATP and decreases AMP [5]. Modulation of Dopamine release [6]. Increases IP level (Sherman).
  
  
• Toxicity (LD₅₀) : mice (orally): 275 mg/kg
  
  
• Storage recommendations : store at room temperature. Solution for use: dissolve in water: 10-³M (2 mg in 6.56 ml), stable for 1-2 days at 20°C.
  
  
• Safety recommendations : Do not swallow or inhale; avoid eye and skin contact.
  
  
• CAS Reg. No. : 79-55-0 (base), 546-48-5 (tartrate), 6152-93-8 (tosilate).
  
  
• Merck Index 11th Ed. : 7022
  
  
• Bibliography :
  
  1. Lee J.E. et al., Nature (1958) 181:1717
  2. Romano C. et al, Psychopharmacologie (1981) 74(4):310-315
  3. Mader et al., "Voltage dependent blocade of a crustacean muscle", J. Exp. Biol. (1980). 88:147-159
  4. Lingle, J. Physio. (1983) (London). 339:419-437
  5. Tichonenko V.M., Farm.Toxikol.(Kiev) (1980). (13):109-125 (1978); [p.42-44 Engl.]., CA 93: 762
  6. Rapier C. et al., Neuropharm. (1990). 54(3):937-945
  7. Spinks et al., Nature (1958). 181:1397
  8. Corne et al., Brit.J.Pharm. (1958). 13(5):501-520
  9. Spinks et al., Brit.J.Pharm. (1958). 13(4):501-520