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Chemical Compound Review

AG-J-87891     (7-hydroxy-8-methyl-8- azabicyclo[3.2.1]oct...

Synonyms: CCG-18441, STOCK1N-72606, BBL012335, CTK8A1522, STK064395, ...
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Disease relevance of anisodamine


High impact information on anisodamine

  • Anisodamine proved a modest inhibitor of granulocyte aggregation and a powerful inhibitor of platelet aggregation; thromboxane synthesis was inhibited in anisodamine-treated platelets, further suggesting that the biochemical mode of action might be inhibition of cyclo-oxygenase or thromboxane synthetase [5].
  • Anisodamine causes acyl chain interdigitation in phosphatidylglycerol [6].
  • At 3 mM anisodamine, the delta H of DPPG reaches 9.6 kcal/mol [6].
  • It is concluded that both anisodamine and to a lesser extent anisodine possess alpha 1-adrenoceptor blocking properties; this antagonistic activity of anisodamine may contribute to its salutary effects on the microcirculation [7].
  • This study demonstrated a direct cardiac depressive action of anisodamine at the myocyte level, which may be related to, at least in part, NO production and cholinoceptor antagonism [8].

Chemical compound and disease context of anisodamine


Biological context of anisodamine

  • Pretreatment with anisodamine increased heart rate from 163 +/- 15 to 289 +/- 10 beats.min-1 and cardiac index from 195 +/- 15 to 238 +/- 14 before endotoxin infusion [14].
  • Thus, the beneficial effect of anisodamine probably is not due to vasodilation of the splanchnic vasculature [1].
  • Various agents have been applied to lower peripheral resistance and cardiac workload, one of which, anisodamine, is widely used in Asia. However, the direct action of anisodamine on cardiac contractile property is essentially unknown [8].
  • In order to investigate the enantiomeric pharmacokinetics and biotransformation of synthetic anisodamine (654-2), a cholinoceptor antagonist widely used in clinic in China, it has been preparatively separated into two racemates (I and II) by using ZORBAX Eclipse XDB-C18 column [15].
  • Anisodamine dose-dependently inhibited this LPS-induced upregulation of PAI-1 and TF [16].

Anatomical context of anisodamine


Associations of anisodamine with other chemical compounds

  • The non-interdigitated DPPG multilamellar vesicles formed in HEPES buffer show clear fluidity gradient in their acyl chains, whereas the fluidity gradients are completely abolished in the presence of anisodamine [6].
  • Anisodamine inhibits cardiac contraction and intracellular Ca(2+) transients in isolated adult rat ventricular myocytes [8].
  • Results showed that the maximum inhibitory rates of Sco, Atr, AT(3), and Ani on gastric emptying and small intestinal movement were 29.78, 40.69, 12.30, and 17.99% and 51.98, 58.46, 46.51, and 46.22%, respectively [18].
  • In this study we aimed to investigate whether the therapeutic efficacy of anisodamine in the treatment of bacteraemic shock could--at least in part--be brought about by its direct interference with the lipopolysaccharide (LPS)-induced activation of endothelial cells [16].
  • The effects of anisodamine on acetylcholine-induced endothelium-dependent relaxation were studied in organ chambers and under bioassay conditions [19].

Gene context of anisodamine


Analytical, diagnostic and therapeutic context of anisodamine


  1. Beneficial effect of anisodamine in hemorrhagic shock. Su, J., Hock, C.E., Lefer, A.M. Naunyn Schmiedebergs Arch. Pharmacol. (1984) [Pubmed]
  2. Protective effect of anisodamine on cultured bovine pulmonary endothelial cell injury induced by oxygen-free radicals. Luo, Z.Y., Tang, Y., You, J.I., Luo, H. Archives of surgery (Chicago, Ill. : 1960) (1992) [Pubmed]
  3. Protective effect of anisodamine on reperfusion injury of skeletal muscles in rabbit. Wei, X., Zhang, Z., Han, L., Wei, Y. Acta orthopaedica Scandinavica. (1998) [Pubmed]
  4. Protective effect of anisodamine against Shiga toxin-1: inhibition of cytokine production and increase in the survival of mice. Zhang, H.M., Ou, Z.L., Gondaira, F., Ohmura, M., Kojio, S., Yamamoto, T. J. Lab. Clin. Med. (2001) [Pubmed]
  5. Anisodamine inhibits thromboxane synthesis, granulocyte aggregation, and platelet aggregation. A possible mechanism for its efficacy in bacteremic shock. Xiu, R.J., Hammerschmidt, D.E., Coppo, P.A., Jacob, H.S. JAMA (1982) [Pubmed]
  6. Anisodamine causes acyl chain interdigitation in phosphatidylglycerol. Wang, P.Y., Chen, J.W., Hwang, F. FEBS Lett. (1993) [Pubmed]
  7. Adrenoceptor blocking properties of atropine-like agents anisodamine and anisodine on brain and cardiovascular tissues of rats. Varma, D.R., Yue, T.L. Br. J. Pharmacol. (1986) [Pubmed]
  8. Anisodamine inhibits cardiac contraction and intracellular Ca(2+) transients in isolated adult rat ventricular myocytes. Norby, F.L., Ren, J. Eur. J. Pharmacol. (2002) [Pubmed]
  9. The effects of anisodamine and dobutamine on gut mucosal blood flow during gut ischemia/ reperfusion. Hu, S., Sheng, Z.Y. World J. Gastroenterol. (2002) [Pubmed]
  10. Delayed thromboxane synthesis inhibition, but not cholinergic blockade, reverses group B streptococcus-induced pulmonary hypertension. Li, J.X., Gray, B.M., Oliver, J.R., Lu, C.Y., Philips, J.B. Developmental pharmacology and therapeutics. (1992) [Pubmed]
  11. Anisodamine as an effective drug to treat snakebites. Li, Q.B., Pan, R., Wang, G.F., Tang, S.X. Journal of natural toxins. (1999) [Pubmed]
  12. Effects of anisodamine on plasma levels of thromboxane B2 (TXB2) and 6-keto-prostaglandin F1 alpha (6-keto-PGF1 alpha) in rat with septic shock. Tao, Y.P., Xiao, D.M., Chen, H.C. Proceedings of the Chinese Academy of Medical Sciences and the Peking Union Medical College = Chung-kuo i hsüeh k'o hsüeh yüan, Chung-kuo hsieh ho i k'o ta hsüeh hsüeh pao. (1988) [Pubmed]
  13. Hemodynamic and nonhemodynamic mechanisms of experimental pulmonary edema in rats and the effect of anisodamine and tetramethylpyrazine. Part 1: Survival rate, pulmonary index, pathological change and pulmonary vascular permeability. Dai, S., Xue, Q., Sun, R., Wang, S., Li, C., Wu, Y., Si, Q., Hu, S. Chin. Med. Sci. J. (1993) [Pubmed]
  14. Effects of cholinergic blockade on hemodynamic disturbances and intestinal lesions in endotoxic shock in newborn piglets. Li, J.X., Kelly, D.R., Oliver, J.R., Grantham, K.D., Philips, J.B. Shock (1994) [Pubmed]
  15. Diastereomeric and enantiomeric high-performance liquid chromatographic separation of synthetic anisodamine. Yang, L.M., Xie, Y.F., Chen, H.Z., Lu, Y. Journal of pharmaceutical and biomedical analysis (2007) [Pubmed]
  16. Anisodamine counteracts lipopolysaccharide-induced tissue factor and plasminogen activator inhibitor-1 expression in human endothelial cells: contribution of the NF-kappa b pathway. Ruan, Q.R., Zhang, W.J., Hufnagl, P., Kaun, C., Binder, B.R., Wojta, J. J. Vasc. Res. (2001) [Pubmed]
  17. Specific inhibitory action of anisodamine against a staphylococcal superantigenic toxin, toxic shock syndrome toxin 1 (TSST-1), leading to down-regulation of cytokine production and blocking of TSST-1 toxicity in mice. Nakagawa, S., Kushiya, K., Taneike, I., Imanishi, K., Uchiyama, T., Yamamoto, T. Clin. Diagn. Lab. Immunol. (2005) [Pubmed]
  18. Comparison of the inhibitory efficacy of four belladonna drugs on gastrointestinal movement and cognitive function in food-deprived mice. Pan, S.Y., Han, Y.F. Pharmacology (2004) [Pubmed]
  19. Anisodamine inhibits acetylcholine-induced endothelium-dependent relaxation of canine femoral artery. Guo, H.Y., Loren, R.R., Vanhutte, P.M. Chin. Med. J. (1992) [Pubmed]
  20. Anisodamine inhibits shiga toxin type 2-mediated tumor necrosis factor-alpha production in vitro and in vivo. Zhang, H.M., Ou, Z.L., Yamamoto, T. Exp. Biol. Med. (Maywood) (2001) [Pubmed]
  21. Anisodamine restores bowel circulation in burn shock. Sheng, C.Y., Gao, W.Y., Guo, Z.R., He, L.X. Burns : journal of the International Society for Burn Injuries. (1997) [Pubmed]
  22. Reduction of granulocyte-mediated lung injury in canine cardiopulmonary bypass by anisodamine infusion. Gu, Y.J., Wang, Y.S., Chiang, B.Y., Gao, X.D., Ye, C.X., Wildevuur, C.R. The Thoracic and cardiovascular surgeon. (1991) [Pubmed]
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