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ION CHANNEL and RECEPTOR LIGANDS TOXINS & ALKALOIDS

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| | L9046 TEMPIDONE
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| PRICES |
| Quantity | US Dollars | EURO |
5 mg | 81.20 | 58.00 |
25 mg | 324.80 | 232.00 |
- 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 :
- Brehteric et al., Nature (1959). 184:1707-1709
- Chodera A. et al., Pharm. Zentralhalle (1964). 103(1):17-23
- Rojas R.L., Rev. Cubana Farm. (1979). 13:37-45 and 163-173
- Rojas R.L., Rev. Cubana Farm. (1979). 16:146-156
- Komarov P.G. et al., Dokl. Akad. Nauk SSSR (1987). 297(3):734-737
- Brito et al., Rev. Cubana Farm. (1982). 16(2):146-156
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