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.

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].

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).

Do not swallow; avoid extra-large quantity inhalation.