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Home Page > Alphabetical Index > TEMPIDONE

TEMPIDONE Prod. No L9046 - CAS # 826-36-8
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Product Name TEMPIDONE
(Syn.: Triacetonamine‚ Vincubine‚ TMP=O)
Product Code L9046
TEMPIDONE

C9H17NO .HCl
Molecular Formula C9H17NO .HCl
Description

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.
 
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].
 
Chemical and Physical Properties
 
CAS No. 826-36-8 Molecular Weight 191.70 Da.
RTECS Physical Form colorless crystal powder.
Merck Index No (13th Ed.) Melting point 195-196 °C.
PubChem SID Solubility water‚ ethanol.
Purity min. 99.5%.

TLC (Silufol UV-254‚ MeOH:NH3(25%) Rf 0.41‚ development with Dragendorff¨ reagent); NMR (D2O).		 Optical Activity
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
Chemical Names 2‚2‚6‚6-tetramethylpiperidone-4 hydrochloride.
Storage & Reconstitution 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.
Safety Recommendations
 
Bibliographic References
  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
 
Prices
Code
Quantity
US $
€uro
L9046
5 mg
81.20
58.00
25 mg
324.80
232.00
 
External Links PubMed Biomedical Citations From PubMed Toxicology Citations From PubMed PubChem SID

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