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Chemical Compound Review

cocaine     methyl (2R,3S)-8-methyl-3...

Synonyms: Blizzard, Cocktail, Delcaine, Goofball, Kokayeen, ...
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Disease relevance of cocaine

  • Although the pathogenesis of cardiac toxicity of cocaine remains incompletely defined, available circumstantial evidence suggests that cocaine has medical consequences that are equal in importance to its well-documented psychosocial consequences [1].
  • Only 4 of 1009 women (0.4 percent) reported ever injecting drugs, and the 4 were HIV-seronegative; however, 14 of 43 users of "crack" cocaine (33 percent) had HIV infection [2].
  • Coronary-artery spasm and myocardial infarction associated with cocaine use [3].
  • No patient had chest pain or ischemic electrocardiographic changes after cocaine use or smoking [4].
  • We identified 39 patients seen at our institution over an eight-year period with acute rhabdomyolysis after cocaine use [5].

Psychiatry related information on cocaine


High impact information on cocaine


Chemical compound and disease context of cocaine


Biological context of cocaine


Anatomical context of cocaine


Associations of cocaine with other chemical compounds

  • In particular, screening of genetically modified mice lacking individual GRKs or beta arrestins for alterations in behavioral and biochemical responses to cocaine and morphine has revealed a functional specificity in dopamine and mu-opioid receptor regulation of locomotion and analgesia [27].
  • Here we examine the effects of cocaine in mice lacking one of the serotonin-receptor subtypes, the 5-HT1B receptor [28].
  • In contrast, chronic exposure to cocaine does not induce these proteins, but instead causes the persistent expression of highly stable isoforms of deltaFosB. deltaFosB is also induced in the nucleus accumbens by repeated exposure to other drugs of abuse, including amphetamine, morphine, nicotine and phencyclidine [29].
  • Indeed, viral-mediated overexpression of both GluR1 and GluR2 in nucleus accumbens shell neurons facilitates extinction of cocaine- but not sucrose-seeking responses [25].
  • Furthermore, the selective CB1 receptor antagonist, SR141716A (ref. 14), attenuates relapse induced by re-exposure to cocaine-associated cues or cocaine itself, but not relapse induced by exposure to stress [30].

Gene context of cocaine

  • A single extinction training session, when conducted during GluR subunit overexpression, attenuates stress-induced relapse to cocaine seeking even after GluR overexpression declines [25].
  • Regulation of gene expression and cocaine reward by CREB and DeltaFosB [31].
  • In contrast, at the BDNF and Cdk5 promoters, genes that are induced by chronic, but not acute, cocaine, H3 hyperacetylation was observed with chronic cocaine only [32].
  • Members of the Homer gene family are regulated by acute and chronic cocaine administration [33].
  • We demonstrate a robust association between cocaine dependence and a VNTR allele in SLC6A3, conferring a small but detectable effect, and we show that this VNTR may be functional [34].

Analytical, diagnostic and therapeutic context of cocaine


  1. Acute cardiac events temporally related to cocaine abuse. Isner, J.M., Estes, N.A., Thompson, P.D., Costanzo-Nordin, M.R., Subramanian, R., Miller, G., Katsas, G., Sweeney, K., Sturner, W.Q. N. Engl. J. Med. (1986) [Pubmed]
  2. Heterosexually transmitted human immunodeficiency virus infection among pregnant women in a rural Florida community. Ellerbrock, T.V., Lieb, S., Harrington, P.E., Bush, T.J., Schoenfisch, S.A., Oxtoby, M.J., Howell, J.T., Rogers, M.F., Witte, J.J. N. Engl. J. Med. (1992) [Pubmed]
  3. Coronary-artery spasm and myocardial infarction associated with cocaine use. Schachne, J.S., Roberts, B.H., Thompson, P.D. N. Engl. J. Med. (1984) [Pubmed]
  4. Coronary-artery vasoconstriction induced by cocaine, cigarette smoking, or both. Moliterno, D.J., Willard, J.E., Lange, R.A., Negus, B.H., Boehrer, J.D., Glamann, D.B., Landau, C., Rossen, J.D., Winniford, M.D., Hillis, L.D. N. Engl. J. Med. (1994) [Pubmed]
  5. Acute rhabdomyolysis associated with cocaine intoxication. Roth, D., Alarcón, F.J., Fernandez, J.A., Preston, R.A., Bourgoignie, J.J. N. Engl. J. Med. (1988) [Pubmed]
  6. Violent injuries among women in an urban area. Grisso, J.A., Schwarz, D.F., Hirschinger, N., Sammel, M., Brensinger, C., Santanna, J., Lowe, R.A., Anderson, E., Shaw, L.M., Bethel, C.A., Teeple, L. N. Engl. J. Med. (1999) [Pubmed]
  7. The use of legal action in New York City to ensure treatment of tuberculosis. Gasner, M.R., Maw, K.L., Feldman, G.E., Fujiwara, P.I., Frieden, T.R. N. Engl. J. Med. (1999) [Pubmed]
  8. Cocaine and Tourette's syndrome. Mesulam, M.M. N. Engl. J. Med. (1986) [Pubmed]
  9. Suppression of psychoactive effects of cocaine by active immunization. Carrera, M.R., Ashley, J.A., Parsons, L.H., Wirsching, P., Koob, G.F., Janda, K.D. Nature (1995) [Pubmed]
  10. Buprenorphine suppresses cocaine self-administration by rhesus monkeys. Mello, N.K., Mendelson, J.H., Bree, M.P., Lukas, S.E. Science (1989) [Pubmed]
  11. moody encodes two GPCRs that regulate cocaine behaviors and blood-brain barrier permeability in Drosophila. Bainton, R.J., Tsai, L.T., Schwabe, T., DeSalvo, M., Gaul, U., Heberlein, U. Cell (2005) [Pubmed]
  12. Cocaine, smoking, and spontaneous abortion. Mills, J.L. N. Engl. J. Med. (1999) [Pubmed]
  13. Cocaine-associated myocardial ischemia. Blaho, K., Merigian, K., Winbery, S. N. Engl. J. Med. (1996) [Pubmed]
  14. Appetite-suppressant drugs and the risk of primary pulmonary hypertension. International Primary Pulmonary Hypertension Study Group. Abenhaim, L., Moride, Y., Brenot, F., Rich, S., Benichou, J., Kurz, X., Higenbottam, T., Oakley, C., Wouters, E., Aubier, M., Simonneau, G., Bégaud, B. N. Engl. J. Med. (1996) [Pubmed]
  15. Fatal injuries after cocaine use as a leading cause of death among young adults in New York City. Marzuk, P.M., Tardiff, K., Leon, A.C., Hirsch, C.S., Stajic, M., Portera, L., Hartwell, N., Iqbal, M.I. N. Engl. J. Med. (1995) [Pubmed]
  16. Use of phentolamine for cocaine-induced myocardial ischemia. Hollander, J.E., Carter, W.A., Hoffman, R.S. N. Engl. J. Med. (1992) [Pubmed]
  17. Cocaine and tobacco use and the risk of spontaneous abortion. Ness, R.B., Grisso, J.A., Hirschinger, N., Markovic, N., Shaw, L.M., Day, N.L., Kline, J. N. Engl. J. Med. (1999) [Pubmed]
  18. Migrainelike headache and cocaine use. Satel, S.L., Gawin, F.H. JAMA (1989) [Pubmed]
  19. Risk of sexually transmitted disease among black adolescent crack users in Oakland and San Francisco, Calif. Fullilove, R.E., Fullilove, M.T., Bowser, B.P., Gross, S.A. JAMA (1990) [Pubmed]
  20. Cerebral vasculitis associated with cocaine abuse. Kaye, B.R., Fainstat, M. JAMA (1987) [Pubmed]
  21. Cocaine-induced coronary-artery vasoconstriction. Lange, R.A., Cigarroa, R.G., Yancy, C.W., Willard, J.E., Popma, J.J., Sills, M.N., McBride, W., Kim, A.S., Hillis, L.D. N. Engl. J. Med. (1989) [Pubmed]
  22. Cocaine use in pregnancy. Chasnoff, I.J., Burns, W.J., Schnoll, S.H., Burns, K.A. N. Engl. J. Med. (1985) [Pubmed]
  23. Pneumopericardium from cocaine inhalation. Adrouny, A., Magnusson, P. N. Engl. J. Med. (1985) [Pubmed]
  24. Cocaine-induced coronary-artery dissection. Jaffe, B.D., Broderick, T.M., Leier, C.V. N. Engl. J. Med. (1994) [Pubmed]
  25. Extinction-induced upregulation in AMPA receptors reduces cocaine-seeking behaviour. Sutton, M.A., Schmidt, E.F., Choi, K.H., Schad, C.A., Whisler, K., Simmons, D., Karanian, D.A., Monteggia, L.M., Neve, R.L., Self, D.W. Nature (2003) [Pubmed]
  26. Single cocaine exposure in vivo induces long-term potentiation in dopamine neurons. Ungless, M.A., Whistler, J.L., Malenka, R.C., Bonci, A. Nature (2001) [Pubmed]
  27. Desensitization of G protein-coupled receptors and neuronal functions. Gainetdinov, R.R., Premont, R.T., Bohn, L.M., Lefkowitz, R.J., Caron, M.G. Annu. Rev. Neurosci. (2004) [Pubmed]
  28. Increased vulnerability to cocaine in mice lacking the serotonin-1B receptor. Rocha, B.A., Scearce-Levie, K., Lucas, J.J., Hiroi, N., Castanon, N., Crabbe, J.C., Nestler, E.J., Hen, R. Nature (1998) [Pubmed]
  29. Expression of the transcription factor deltaFosB in the brain controls sensitivity to cocaine. Kelz, M.B., Chen, J., Carlezon, W.A., Whisler, K., Gilden, L., Beckmann, A.M., Steffen, C., Zhang, Y.J., Marotti, L., Self, D.W., Tkatch, T., Baranauskas, G., Surmeier, D.J., Neve, R.L., Duman, R.S., Picciotto, M.R., Nestler, E.J. Nature (1999) [Pubmed]
  30. A cannabinoid mechanism in relapse to cocaine seeking. De Vries, T.J., Shaham, Y., Homberg, J.R., Crombag, H., Schuurman, K., Dieben, J., Vanderschuren, L.J., Schoffelmeer, A.N. Nat. Med. (2001) [Pubmed]
  31. Regulation of gene expression and cocaine reward by CREB and DeltaFosB. McClung, C.A., Nestler, E.J. Nat. Neurosci. (2003) [Pubmed]
  32. Chromatin remodeling is a key mechanism underlying cocaine-induced plasticity in striatum. Kumar, A., Choi, K.H., Renthal, W., Tsankova, N.M., Theobald, D.E., Truong, H.T., Russo, S.J., Laplant, Q., Sasaki, T.S., Whistler, K.N., Neve, R.L., Self, D.W., Nestler, E.J. Neuron (2005) [Pubmed]
  33. Homer proteins regulate sensitivity to cocaine. Szumlinski, K.K., Dehoff, M.H., Kang, S.H., Frys, K.A., Lominac, K.D., Klugmann, M., Rohrer, J., Griffin, W., Toda, S., Champtiaux, N.P., Berry, T., Tu, J.C., Shealy, S.E., During, M.J., Middaugh, L.D., Worley, P.F., Kalivas, P.W. Neuron (2004) [Pubmed]
  34. A dopamine transporter gene functional variant associated with cocaine abuse in a Brazilian sample. Guindalini, C., Howard, M., Haddley, K., Laranjeira, R., Collier, D., Ammar, N., Craig, I., O'Gara, C., Bubb, V.J., Greenwood, T., Kelsoe, J., Asherson, P., Murray, R.M., Castelo, A., Quinn, J.P., Vallada, H., Breen, G. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  35. Disability income, cocaine use, and repeated hospitalization among schizophrenic cocaine abusers--a government-sponsored revolving door? Shaner, A., Eckman, T.A., Roberts, L.J., Wilkins, J.N., Tucker, D.E., Tsuang, J.W., Mintz, J. N. Engl. J. Med. (1995) [Pubmed]
  36. The prevalence of illicit-drug or alcohol use during pregnancy and discrepancies in mandatory reporting in Pinellas County, Florida. Chasnoff, I.J., Landress, H.J., Barrett, M.E. N. Engl. J. Med. (1990) [Pubmed]
  37. Routes of infection, viremia, and liver disease in blood donors found to have hepatitis C virus infection. Conry-Cantilena, C., VanRaden, M., Gibble, J., Melpolder, J., Shakil, A.O., Viladomiu, L., Cheung, L., DiBisceglie, A., Hoofnagle, J., Shih, J.W. N. Engl. J. Med. (1996) [Pubmed]
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