Disease relevance of Secoverine

• The effect of secoverine hydrochloride on stimulated sigmoid motility: a double-blind, placebo controlled cross-over study in irritable bowel syndrome [1].

High impact information on Secoverine

• In particular, the rank of potencies for the drugs tested was: atropine greater than secoverine greater than stercuronium greater than pirenzepine at the autoreceptors, both in cortex and hippocampus; but it was: atropine greater than pirenzepine = secoverine greater than stercuronium, at the heteroreceptors in the striatum [2].
• Inhibition of gastric acid secretion by atropine and secoverine occurred at a similar dose-range (10(-9) and 2 X 10(-9) M) [3].
• Both atropine and secoverine inhibited cholinergically induced gastric acid secretion and gastric motility [3].
• A series of 8 muscarinic antagonists was used with preference for M1 receptors (telenzepine and pirenzepine), M1 and M2 receptors (secoverine), M2 receptors (AF-DX 116 and himbacine) and M1 and M3 receptors (p-F-HHSiD and HHSiD) [4].
• Among the anticholinergic drugs, oxybutynin had a significantly lower value for the inhibition constant (Ki) in the submandibular gland whereas Ki for both secoverine and pirenzepine was significantly higher in this tissue than in urinary bladder [5].

Biological context of Secoverine

• At very high concentrations secoverine recognized an allosteric site on the muscarinic receptors and reduced the dissociation rates of the 3H-ligands [6].
• At concentrations between 10(-6) and 10(-3) M, secoverine interaction with an additional receptor site resulted in profound changes of tracer kinetics, suggesting the formation of a ternary complex (secoverine-radioligand-muscarinic receptor) [6].
• 3. By contrast, secoverine had only marginal effects on the sphincter and ciliary muscle of the eye, almost no effect on cholinergically-induced salivation and lacrimation, gastric acid production, urinary bladder function, gastric emptying or normal peristalsis [7].

Anatomical context of Secoverine

• The mean values for the inhibition constant (Ki) were significantly lower for oxybutynin, amitriptyline, and pirenzepine but higher for secoverine in preparations of the urinary bladder than of the parotid gland [8].
• The effect of secoverine on colonic smooth muscle was measured in patients with diverticular disease and in healthy subjects [9].
• The selective muscarinic receptor antagonist secoverine was found to have a similar affinity for muscarinic receptors in the guinea-pig left atrium and ileal longitudinal muscle as well as in the rat urinary bladder and ileum [10].
• The actions of secoverine and atropine on bethanechol-induced intestinal secretion, hypermotility and transintestinal potential difference were investigated in the rat jejunum in-vivo [11].
• 1. In in vitro experiments the competitive antagonism of secoverine against muscarinomimetics was demonstrated on guinea pig ileum, rat jejunum and calif trachea smooth muscle [7].

Analytical, diagnostic and therapeutic context of Secoverine

• 5. Secoverine did not cause ulceration of the stomach wall of the rat during acute or prolonged oral administration of high doses [12].

References