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Chemical Compound Review

Secoverina     1-cyclohexyl-4-[ethyl-[1-(4...

Synonyms: Secoverine, secovorine, Secoverinum, SureCN457590, CHEMBL2105414, ...
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Disease relevance of Secoverine


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


Analytical, diagnostic and therapeutic context of Secoverine


  1. The effect of secoverine hydrochloride on stimulated sigmoid motility: a double-blind, placebo controlled cross-over study in irritable bowel syndrome. Ehsanullah, M., Lee, D.A., Williams, T., Pollard, P., Gazzard, B. British journal of clinical pharmacology. (1985) [Pubmed]
  2. Heterogeneity of presynaptic muscarinic receptors regulating neurotransmitter release in the rat brain. Raiteri, M., Leardi, R., Marchi, M. J. Pharmacol. Exp. Ther. (1984) [Pubmed]
  3. The effects of atropine and secoverine on gastric secretion and motility in the mouse isolated stomach. Davison, J.S., Greenwood, B., Najafi-Farashah, A., Read, N.W. Br. J. Pharmacol. (1983) [Pubmed]
  4. Characterization of the muscarine receptor type on paracrine cells activated by McN-A-343 in the mouse isolated stomach. Kromer, W., Baron, E., Beinborn, M., Boer, R., Eltze, M. Naunyn Schmiedebergs Arch. Pharmacol. (1990) [Pubmed]
  5. Comparison of muscarinic acetylcholine binding in the urinary bladder and submandibular gland of the rabbit. Batra, S. Eur. J. Pharmacol. (1987) [Pubmed]
  6. Secoverine is a non-selective muscarinic antagonist on rat heart and brain receptors. Brunner, F., Waelbroeck, M., Christophe, J. Eur. J. Pharmacol. (1986) [Pubmed]
  7. Pharmacology of secoverine, a new spasmolytic agent with specific antimuscarinic properties. Part 1: Antimuscarinic and spasmolytic effects. Zwagemakers, J.M., Claassen, V. Arzneimittel-Forschung. (1980) [Pubmed]
  8. Identification and characterization of muscarinic cholinergic receptors in the human urinary bladder and parotid gland. Batra, S., Biörklund, A., Hedlund, H., Andersson, K.E., Björklund, A. J. Auton. Nerv. Syst. (1987) [Pubmed]
  9. Effect of secoverine on colonic myoelectric activity in diverticular disease of the colon. Suchowiecky, M., Clarke, D.D., Bhasker, M., Perry, R.J., Snape, W.J. Dig. Dis. Sci. (1987) [Pubmed]
  10. Comparison of the affinity of secoverine for some muscarinic receptors. Choo, L.K., Mitchelson, F. Clin. Exp. Pharmacol. Physiol. (1985) [Pubmed]
  11. Effect of secoverine and atropine on intestinal secretion and motor activity in the rat small intestine in-vivo. Greenwood, B., Read, N.W., Hardcastle, P.T., Hardcastle, J. J. Pharm. Pharmacol. (1984) [Pubmed]
  12. Pharmacology of secoverine, a new spasmolytic agent with specific antimuscarinic properties. Part 2: General pharmacological properties. Zwagemakers, J.M., Claassen, V. Arzneimittel-Forschung. (1980) [Pubmed]
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