BICARPHEN
Product ID L9032 
Name BICARPHEN 
Molecular formula C22H27NO.HCl.2H2O
Description

It is a semirigid molecular probe for different ion channels or receptors, specifically a Na+ channels blocker.
It represents a new class of anti-histaminic (nonH1 or H2) and anti 5-HT anti-allergic drugs: potential antagonist of H-3 histamine and serotonine (non 5-HT2) receptors.

It is also an anti-pruritic and a diamine oxidase activator.


Quinuclidine derivative, synthetic
Biological activity

Ion channels agent:
On Na+ channels (CA1-CA3 region of rat hippocampus neurons), 2.5x10-4 M results in 100 % blocking effect, 2x10-6 M in 50%.
On isolated throat ganglia neurons of the snail Limnea stagnalis (patch-clamp whole-cell recording):
* On K+ channels: meagre reversible blockade at 10-5 M.
* No effect on Ca2+ or Cl- channels.

Anti-allergic.
Non-sedative low anti-cholinergic anti-histaminic of prolonged action combined with anti-serotonine activity: aerosol histamine bronchoconstriction prevention in guinea-pig : 80-90 % at 2 mg/kg, the same for 5-HT : > 2 mg/kg. (Phencarol: 0.2 and 1 mg/kg respectively). Prolonged action (3-4 hours) and enhanced anti-5-HT activity compared to Phencarol (1.5 hours); efficient against itches. Non H-1, H-2 or 5-HT2 blocker: no binding to rat cortex H-1, H-2 receptors, 5-HT-2 receptors.

Low affinity to M-AChR.
pIC50 [3H]-quinuclidinyl-3-benzylate, rat brain (M-1)/heart (M-2) 5.63/5.33; guinea pig ileum 4.9 (Methylfurmethide), 5.5 (ACh); Pridinol 7.3/6.8, Atropine 9.0/10.0.
Good penetration of biological membranes.
Diamine oxidase activator (75 mg/kg p.o., rat lung, 60 min +52%, 180 min +44%).
weak anti-AChE activity in vitro (human erythrocytes) Ki. 104 = 2.60, type of inhibition: mixed competitive/non competitive.

 Packaging and Prices

Packaging Price (€) Quantité Buy Now
5 mg 808.00

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 Product Technical Documents
Safety Data Sheet Available on request, please Contact us
Ref. SDS_L9032 : unit price : free of charge
 Chemical and Physical Properties
Product code L9032  Molecular weight 393.96 g/mol
Product name BICARPHEN  Physical form colorless crystal powder
CAS No. 57734-70-0 Melting point 277-279 °C (dec).
RTECS CL5627600 Solubility Sparingly in water (25 °C, 4 mM)
Better in 50 % ethanol
UNIPROT Optical Activity No optical Activity
PubChem SID    
PubChem CID 50853316    
Purity min. 98 %.
(TLC [on Silufol UV-254 - MeOH-NH3 (25 %) 10:1, Rf = 0.14. Visualization by UV-light followed by Dragendorff's reagent.], NMR[CD3OD])
   
Toxicity(LD50) mice (p.o.): 650 mg/kg.
mice (i.v.): 68 mg/kg
   
Chemical Name 1-azabicyclo[2.2.2]octan-3-yl-bis(2-methylphenyl)methanol;hydrochloride    
Storage & Reconstitution
Recommandations

Stable in dry state and solution (up to 150 °C).
Dissolves slowly, use heating or boiling. Solution for use: 10-3 M (2 mg in 5.01 ml).


 
Savety Recommandations

Do not swallow, avoid extra-large quantity inhalation.
 For research use only — not intended for food, diagnostic or therapeutic use

 
 Bibliographic References
Product code L9032 
Product name BICARPHEN 

- Kaminka M.E. et al., Khim. Farm. Zh. (1976). 10(9):22-27
- Kaminka M.E. et al., Drugs of Today (1988). 24(10):701-703
- Kaminka M.E. et al., Farm. Toksikol (1988) (Russian). (2):21-26
- Gankina E.M. et al., Eksp. Klin. Farmacol. (1993) (Russian). (1):22-24
- Baumanis E.A. et al., Farm. Toksikol (1980) (Russian). (1):36-41
- Mashkovsky M.D. et al., "Further developments in research on the chemistry and pharmacology of synthetic quinuclidine derivatives." Progr. Drug. Res., (1983). 27:9-61
 Links
Product code L9032 
Product name BICARPHEN 
External Links PubMed
Biomedical Citations From PubMed
Toxicology Citations From PubMed
PubChem CID
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