Summary: An acaricide used against many organophosphate and carbamate resistant pests. It acts as an uncoupling agent and monoamine oxidase inhibitor.

Top Publications

  1. Alemany R, Olmos G, García Sevilla J. The effects of phenelzine and other monoamine oxidase inhibitor antidepressants on brain and liver I2 imidazoline-preferring receptors. Br J Pharmacol. 1995;114:837-45 pubmed
  2. Altobelli D, Martire M, Maurizi S, Preziosi P. Interaction of formamidine pesticides with the presynaptic alpha(2)-adrenoceptor regulating. Toxicol Appl Pharmacol. 2001;172:179-85 pubmed
  3. Wu D, Costa L, Murphy S. [The effect of pesticides-CDM and AMZ on inhibition of the binding of 3H-clonidine to alpha 2-adrenoreceptor in rat forebrain tissue]. Hua Xi Yi Ke Da Xue Xue Bao. 1990;21:17-21 pubmed
    ..Time course and washing test indicated that the inhibition effect by CDM and AMZ was reversible. ..
  4. Ahmed M, Matsumura F. Synergistic actions of formamidine insecticides on the activity of pyrethroids and neonicotinoids against Aedes aegypti (Diptera: Culicidae). J Med Entomol. 2012;49:1405-10 pubmed
    ..These results indicate that amitraz is a promising synergist that shows the potential to increase the efficacy of certain members of type II pyrethroids as well as neonicotinoids to control Ae. aegypti larvae. ..
  5. Cooper R, Barrett M, Goldman J, Rehnberg G, McElroy W, Stoker T. Pregnancy alterations following xenobiotic-induced delays in ovulation in the female rat. Fundam Appl Toxicol. 1994;22:474-80 pubmed
    ..Litter size was not affected if the females were mated on the same day that treatment was administered (0-day delay).(ABSTRACT TRUNCATED AT 250 WORDS) ..
  6. He R, Bai Y. [Effect of scopolamine on the acute severe chlorphenamidine poisoning patients]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2012;30:298-300 pubmed
    To investigate effectiveness of scopolamine on the acute severe chlorphenamidine poisoning patients...
  7. Jimenez J, Bernal J, Toribio L, del Nozal M, Martin M. Capillary gas chromatography with mass spectrometric and atomic emission detection for characterization and monitoring chlordimeform degradation in honey. J Chromatogr A. 2002;946:247-53 pubmed
    ..5% of its initial value; the concentration of compound I increased gradually whereas compound III was present in a larger proportion and reached a maximum around the 14th week. ..
  8. Bjorquist P, Ehnebom J, Inghardt T, Hansson L, Lindberg M, Linschoten M, et al. Identification of the binding site for a low-molecular-weight inhibitor of plasminogen activator inhibitor type 1 by site-directed mutagenesis. Biochemistry. 1998;37:1227-34 pubmed
    ..Moreover, the structure of this region in active PAI-1 has to be different from the corresponding regions in latent and cleaved PAI-1. ..
  9. Watkinson W, Highfill J, Gordon C. Modulating effect of body temperature on the toxic response produced by the pesticide chlordimeform in rats. J Toxicol Environ Health. 1989;28:483-500 pubmed

More Information


  1. He R, Du J, Yang B, Liu B, Duan C, Hu Z, et al. [Effects of treatment with redox agent, blood transfusion and scopolamine on 200 patients with severe chlorphenamidine poisoning]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2003;21:203-5 pubmed
    To verify the effects of treatment with blood transfusion and scopolamine on severe chlorphenamidine poisoning (SCP). 400 patients with severe oral chlorphenamidine poisoning were randomly divided into two groups...
  2. Rien D, Kern R, Kurtz R. Octopaminergic modulation of contrast gain adaptation in fly visual motion-sensitive neurons. Eur J Neurosci. 2012;36:3030-9 pubmed publisher
    ..Contrast gain adaptation could therefore be the basis for a shift in the velocity tuning that was previously suggested to contribute to state-dependent processing of visual motion information in the lobula plate interneurons. ..
  3. Goldman J, Cooper R, Edwards T, Rehnberg G, McElroy W, Hein J. Suppression of the luteinizing hormone surge by chlordimeform in ovariectomized, steroid-primed female rats. Pharmacol Toxicol. 1991;68:131-6 pubmed
    ..This indicates that an indirect adrenal effect was not the principal route, but may accompany an action of CDF on the hypothalamic mechanisms regulating the surge and becomes evident after more prolonged exposure. ..
  4. Brooker A, Grano Maldonado M, Irving S, Bron J, Longshaw M, Shinn A. The effect of octopaminergic compounds on the behaviour and transmission of Gyrodactylus. Parasit Vectors. 2011;4:207 pubmed publisher
    ..salaris infections. With more research there is potential for use of octopaminergic compounds, which have minimal effects on the host or its environment, as parasite-specific treatments against G. salaris infections. ..
  5. Gilbert M, Mack C. Enhanced susceptibility to kindling by chlordimeform may be mediated by a local anesthetic action. Psychopharmacology (Berl). 1989;99:163-7 pubmed
    ..These data provide support for a local anesthetic action of chlordimeform and stand in contrast to several recent demonstrations of alpha-2 activity of formamidines as a primary contributor to formamidine toxicity. ..
  6. Popp W, Schmieding W, Speck M, Vahrenholz C, Norpoth K. Incidence of bladder cancer in a cohort of workers exposed to 4-chloro-o-toluidine while synthesising chlordimeform. Br J Ind Med. 1992;49:529-31 pubmed
    ..7, 53.8, and 35.0 respectively. This provides further evidence that monocyclic aromatic amines such as 4-chloro-o-toluidine may be carcinogenic in humans. ..
  7. Moser V, McCormick J, Creason J, MacPhail R. Comparison of chlordimeform and carbaryl using a functional observational battery. Fundam Appl Toxicol. 1988;11:189-206 pubmed
    ..Body weight and temperature were decreased by both compounds. Thus, the profiles of effect produced by these two pesticides could be clearly differentiated using the FOB...
  8. Gilbert M. Formamidine pesticides enhance susceptibility to kindled seizures in amygdala and hippocampus of the rat. Neurotoxicol Teratol. 1988;10:221-7 pubmed
    ..The alpha-2 adrenergic agonist and/or local anesthetic-like properties of these compounds may be responsible for these seizure enhancing effects. ..
  9. Jurincic C, Horlbeck R, Metz K, Klippel K. [Acute hemorrhagic cystitis following chlordimeform poisoning ]. Dtsch Med Wochenschr. 1991;116:816-8 pubmed
    ..It is likely that chlordimeform had previously been transported in the water-tank. In case of haemorrhagic cystitis possibly caused by occupational or other poisoning, serum and urine should always be obtained for toxicological tests. ..
  10. Vehovszky A, Hiripi L, Elliott C. Octopamine is the synaptic transmitter between identified neurons in the buccal feeding network of the pond snail lymnaea stagnalis. Brain Res. 2000;867:188-99 pubmed
    ..This is the first example of identified octopaminergic synaptic connections within the snail CNS. ..
  11. Goldman J, Stoker T, Perreault S, Cooper R, Crider M. Influence of the formamidine pesticide chlordimeform on ovulation in the female hamster: dissociable shifts in the luteinizing hormone surge and oocyte release. Toxicol Appl Pharmacol. 1993;121:279-90 pubmed
    ..Under the present conditions, this perturbation can be characterized as a delay in the LH trigger, rather than a blockade. ..
  12. Gils A, Stassen J, Nar H, Kley J, Wienen W, Ries U, et al. Characterization and comparative evaluation of a novel PAI-1 inhibitor. Thromb Haemost. 2002;88:137-43 pubmed
    ..In addition, the results stress the necessity for a careful selection of the method used for the evaluation of PAI-1 inhibitors, preferably requiring a panel of screening methods. ..
  13. Hsu W, Smith B, Hollingworth R. The bradycardic and mydriatic effects of chlordimeform and its demethylated analogs in the rat: antagonism by idazoxan but not by prazosin. Life Sci. 1988;43:1897-904 pubmed
  14. Kale P, Petty B, Walker S, Ford J, Dehkordi N, Tarasia S, et al. Mutagenicity testing of nine herbicides and pesticides currently used in agriculture. Environ Mol Mutagen. 1995;25:148-53 pubmed
    ..It is probable that different germ cell stages and treatment regimens are suitable for different types of chemicals. larval treatment may still be valuable and can complement adult treatment in environmental mutagen testing...
  15. Rosenberg L, Glusman J, Libersat F. Octopamine partially restores walking in hypokinetic cockroaches stung by the parasitoid wasp Ampulex compressa. J Exp Biol. 2007;210:4411-7 pubmed
    ..The effect of the octopamine receptor agonist was maximal when injected into the brain, suggesting that the wasp venom interferes with octopaminergic modulation of walking initiation in central structures of the cockroach brain...
  16. Boyes W, Moser V. An alpha 2-adrenergic mode of action of chlordimeform on rat visual function. Toxicol Appl Pharmacol. 1988;92:402-18 pubmed
    ..These results support the hypothesis that chlordimeform alters rat pattern-reversal evoked potentials through actions as a central nervous system alpha 2-adrenergic agonist. ..
  17. Stone J. Content of notification: exposure to the pesticide chlordimeform. Am J Ind Med. 1993;23:93-5 pubmed
  18. Vierk R, Pflueger H, Duch C. Differential effects of octopamine and tyramine on the central pattern generator for Manduca flight. J Comp Physiol A Neuroethol Sens Neural Behav Physiol. 2009;195:265-77 pubmed publisher
    ..Therefore, octopamine and tyramine exert distinct effects on the flight central pattern generating network...
  19. Costa L, Gastel J, Murphy S. The formamidine pesticides chlordimeform and amitraz decrease hepatic glutathione in mice through an interaction with alpha 2-adrenoceptors. J Toxicol Environ Health. 1991;33:349-58 pubmed
    ..These results indicate that formamidine pesticides can affect the levels of hepatic GSH, possibly through a direct interaction with hepatic alpha 2-adrenoceptors. ..
  20. Watkinson W, Gordon C. Caveats regarding the use of the laboratory rat as a model for acute toxicological studies: modulation of the toxic response via physiological and behavioral mechanisms. Toxicology. 1993;81:15-31 pubmed
    ..In general, the rat responds to acute intoxication by lowering its core temperature via both physiological and behavioral mechanisms, thereby attenuating the induced toxicity. Similar responses have not been reported in humans. ..
  21. Costa L, Wu D, Olibet G, Murphy S. Formamidine pesticides and alpha 2-adrenoceptors: studies with amitraz and chlordimeform in rats and development of a radioreceptor binding assay. Neurotoxicol Teratol. 1989;11:405-11 pubmed
  22. Zhou C, Rao Y, Rao Y. A subset of octopaminergic neurons are important for Drosophila aggression. Nat Neurosci. 2008;11:1059-67 pubmed publisher
    ..We carried out genetic rescue experiments that revealed the functional importance of neuronal octopamine and identified a small subset of octopaminergic neurons in the suboesophageal ganglion as being important for aggression. ..
  23. Stevenson P, Dyakonova V, Rillich J, Schildberger K. Octopamine and experience-dependent modulation of aggression in crickets. J Neurosci. 2005;25:1431-41 pubmed
    ..The idea that activity-specific induction of the octopaminergic system underlies other forms of experience-dependent plasticity of aggressive motivation in insects is discussed...
  24. Göggelmann W, Bauchinger M, Kulka U, Schmid E. Genotoxicity of 4-chloro-o-toluidine in Salmonella typhimurium, human lymphocytes and V79 cells. Mutat Res. 1996;370:39-47 pubmed
    ..typhimurium strains TA 100 and TA 98 were about 2-fold higher than those in controls. ..
  25. Ahmed M, Vogel C. The role of octopamine receptor agonists in the synergistic toxicity of certain insect growth regulators (IGRs) in controlling Dengue vector Aedes aegypti (Diptera: Culicidae) mosquito. Acta Trop. 2016;155:1-5 pubmed publisher
    ..aegypti control. However, further field experiments need to be done to understand the unique potential role of OR agonists and their synergistic action on IGRs. ..
  26. Raffa R, Orr N, Connelly C, Hollingworth R. XAMI and DCDM, agonists at cAMP-associated octopamine receptors in cockroach nerve cord, produce centrally mediated antinociception in mice. Brain Res. 1991;559:211-9 pubmed
    ..Mechanistically, XAMI-induced antinociception was antagonized by yohimbine and idazoxan, but not the opiate antagonist naloxone.(ABSTRACT TRUNCATED AT 250 WORDS) ..
  27. Fisher S. Joint action between binary mixtures of chlordimeform and insecticides. Ecotoxicol Environ Saf. 1992;23:11-21 pubmed
    ..Metabolic studies of pairs of compounds using two radiolabeled carbamates showed that CDF altered the metabolic detoxification of both carbaryl and aldicarb. The results suggest that CDF may inhibit MFOs as its mode of action. ..
  28. Chen Z, Lu Z. Sodium dimercaptopropane sulfonate as antidote against non-metallic pesticides. Acta Pharmacol Sin. 2004;25:534-44 pubmed
  29. Thomas W, Craig G, Stacey N. Effects of chlordimeform and its metabolite 4-chloro-o-toluidine on rat splenic T, B and tumoricidal effector cells. Immunopharmacology. 1990;19:79-86 pubmed
  30. Goldman J, Cooper R, Laws S, Rehnberg G, Edwards T, McElroy W, et al. Chlordimeform-induced alterations in endocrine regulation within the male rat reproductive system. Toxicol Appl Pharmacol. 1990;104:25-35 pubmed
  31. Candura S, Marraccini P, Costa L, Manzo L, Rossi A, Coccini T, et al. Calcium entry blockade as a mechanism for chlordimeform-induced inhibition of motor activity in the isolated guinea-pig ileum. Pharmacol Toxicol. 1992;71:426-33 pubmed
    ..On the whole, these results indicate that chlordimeform-induced depression of motor activity in the guinea-pig ileum is, at least in part, related to inhibition of transmembrane Ca2+ fluxes responsible for smooth muscle contraction. ..
  32. Sun B, Liu D, Zhan L. [Rapid method for determination of chlordimeform residue in honey]. Se Pu. 1999;17:93-4 pubmed
    ..The limit of determination is 10 ng. The experiment could be completed in 3 h for a sample without large equipment and special reagent. ..
  33. Vierk R, Duch C, Pflüger H. Postembryonic development of centrally generated flight motor patterns in the hawkmoth, Manduca sexta. J Comp Physiol A Neuroethol Sens Neural Behav Physiol. 2010;196:37-50 pubmed publisher
    ..These findings are discussed in the context of known physiological and structural CNS development during Manduca metamorphosis. ..
  34. Yi X, Han L, Yang H, Fan X, Zhu J, Guo D. [Determination of chlordimeform and its metabolite residues in honey using liquid chromatography-tandem mass spectrometry]. Se Pu. 2010;28:649-53 pubmed
    ..The relative standard deviations were 4.8% - 10.2% and 4.7% -9.1%, respectively. The method can meet the requirements for the determination of chlordimeform and 4-chloro-o-toluidine in honey for import and export inspection. ..
  35. Stoker T, Goldman J, Cooper R, McElroy W. Influence of chlordimeform on alpha-adrenergic receptor-associated mechanisms of hormonal regulation in the rat: pituitary and adrenocortical secretion. Toxicology. 1991;69:257-68 pubmed
    ..These effects indicate that CDF is interfering with a regulatory signal mediated by alpha-adrenergic receptor-associated activity. ..
  36. Leslie C, Reidy G, Murray M, Stacey N. Induction of xenobiotic biotransformation by the insecticide chlordimeform, a metabolite 4-chloro-o-toluidine and a structurally related chemical o-toluidine. Biochem Pharmacol. 1988;37:2529-35 pubmed
    ..Thus each chemical has been shown to induce various pathways of biotransformation with increases in the P-450c and P-450d specific substrate ethoxyresorufin-O-deethylase being a consistent finding. ..
  37. Gordon C, Watkinson W. Behavioral and autonomic thermoregulation in the rat following chlordimeform administration. Neurotoxicol Teratol. 1988;10:215-9 pubmed
    ..The changes in temperature were concomitant with an abrupt drop in heart rate.(ABSTRACT TRUNCATED AT 250 WORDS) ..
  38. Costa L, Olibet G, Murphy S. Alpha 2-adrenoceptors as a target for formamidine pesticides: in vitro and in vivo studies in mice. Toxicol Appl Pharmacol. 1988;93:319-28 pubmed
    ..The results of these biochemical studies support the hypothesis that alpha 2-adrenoceptors represent an important target for formamidine neurotoxicity in mammals. ..
  39. Liu M, Plapp F. Formamidines as synergists of cypermethrin in susceptible and pyrethroid resistant house flies (Diptera: Muscidae). J Econ Entomol. 1990;83:2181-6 pubmed
    ..Both target site and behavioral effects are discussed as possible mechanisms of formamidine synergism of cypermethrin and other pyrethroids. ..