PHENCAROL
Product ID L9031 
Name PHENCAROL 
Molecular formula C20H23NO.HCl
Description

a semirigid molecular probe for different ion channels or receptors. A ligand with activating effect on Cl- channels and blocking effect on K+, Na+ and Ca2+ channels. Potent antiarrhythmic. Represents a new class of anti-histaminic (non H1 or H2) anti-allergic drugs: potential antagonist of H-3 histamine and (non 5-HT-2) serotonine receptors. Diamine oxidase activator. Inhibits gastric secretion.


Quinuclidine derivative, , synthetic.
Biological activity

For detailed information see the attached tables and abstracts.
Ion channels agent.
On Na+ channels (CA1-CA3 region of rat hippocampus neurons), 5x10-4 M results in 100 % blocking effect, 5x10-5 M in 50%.
On isolated throat ganglia neurons of the snail Limnea stagnalis (patch-clamp whole-cell recording):
* On K+ channels, irreversible blockade
-slow currents:10-5 M results in 100% blocking effect and 10-6 M in 40%
-fast currents:10-5 M results in 55% blocking effect.
* On Ca2+ channels:10-6 M results in 60% inhibition of conductivity.
* On Cl- channels: 10-7M results in 170% increase in conductivity.

Anti-allergic.
Non-sedative low anti-cholinergic anti-histaminic drug. Activity: guinea pig ileum, ED50 = 5x10-9 g/ml, pA2 =5.3 (duration of action: 1.5 hours) [1-2]. Non-typical H-blocker (potentially H-3). Low binding to H-1 receptors: competition with [3H] Mepyramine at rat cortex H-1, IC50 = 320 nM, pIC50 = 76 for Diphenhydramine; no binding to H-2 receptors, or to 5HT-2 receptors [3].

Low affinity to M-AChR.
pIC50 [3H]-quinuclidinyl-3-benzylate, rat-brain (M-1)/heart(M-2) 6.36/5.23; guinea pig ileum 6.5 (methylfurmethide), 6.2 (ACh); Pridinol 7.3/6.8, Atropine 9.0/10.0.

Anti-secretory.
Moderately suppresses gastric secretion, the effect is blocked by DAO inhibitor aminoguanidin [4].

Anti-AChE activityin vitro (human erythrocytes) Ki. 104 = 2.33, type of inhibition: competitive.

DAO activator. 50 mg/kg p.o., rat lung, 45 min. +33%, 60 min. + 45%, 180 min. +33% [5].

Extremely efficient anti-arrhythmic. Stops and prevents CaCl2, Strofantin and Adrenaline arrhythmias: rabbits, 5 mg/kg: 100 % in 10-15 seconds; no effect on Aconitine arrhythmia (probably does not bind to site 2 of Na+ channels). Used in emergency clinical practice.

No influence on ECG, pace rate, no cardiodepressive effect [6].
Good penetration of biological membranes.
Low influence on the electrical activity of the brain [2].

 Packaging and Prices

Packaging Price (€) Quantité Buy Now
1 x 1mg 242.00

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5 x 1mg 968.00

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For quotation of big quantities, please Contact us
 Product Technical Documents
Safety Data Sheet Available on request, please Contact us
Ref. SDS_L9031 : unit price : free of charge
 Chemical and Physical Properties
Product code L9031  Molecular weight 329.86 Da.
Product name PHENCAROL  Physical form colorless crystal powder.
CAS No. 10447-39-9 (HCl); 10447-38-9 (base). Melting point 296-298 °C (decomp.).
RTECS Solubility sparingly in water (25°C: 11.6 mM); better in 50% ethanol.
UNIPROT Optical Activity
PubChem SID    
PubChem CID 115027    
Purity min. 98 %.
(TLC [on
   
Toxicity(LD50) mice (orally): 360 mg/kg.
mice (i.v.): 62 mg/kg
   
Chemical Name (3-quinuclidinyl)diphenyl carbinol hydrochloride, (3-quinuclidinyl)diphenyl methanol hydrochloride.    
Storage & Reconstitution
Recommandations

Stable in dry state and in solution up to 100 °C. Dissolves slowly, use heating or boiling. Solution for use: dissolve in water: 10-3 M (2 mg in 6.06 ml).


 
Savety Recommandations

Do not swallow; avoid extra-large quantity inhalation.

 
 Bibliographic References
Product code L9031 
Product name PHENCAROL 

- Mashkovsky M.D. et al., "Further developments in research on the chemistry and pharmacology of synthetic quinuclidine derivatives." Progr. Drug. Res., 27:9-61
- Kaminka M.E. et al., Farm. Toksikol (1977). (2):158-162
- 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
- Kaminka M.E. et al., Bull Exp. Biol. Med. (1993) (Russian). (5):44-46
- Baumanis E.A. et al., Farm. Toksikol (1980) (Russian). (1):36-41
- Yakovlev G.M. et al., Farm. Toksikol (1991) (Russian). (5):25-27
- Tondeur R. et al., Chim. Ther. (1966). 207
- Villany et F.J. al., J. Med. Chem. (1975). 18(7):666-669
 Links
Product code L9031 
Product name PHENCAROL 
External Links PubMed
Biomedical Citations From PubMed
Toxicology Citations From PubMed
PubChem CID
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