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Chemical Compound Review

Metholes     2-amino-3-(3,4- dihydroxyphenyl)-2-methyl...

Synonyms: Mulfasin, DL-Methyldopa, CHEMBL718, SureCN196981, AG-F-93650, ...
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Disease relevance of methyldopa


Psychiatry related information on methyldopa


High impact information on methyldopa


Chemical compound and disease context of methyldopa


Biological context of methyldopa

  • If the blood pressure remained raised, methyldopa was added to the active regimen and matching placebo in the placebo group [17].
  • In addition, acute, intra-arterial administration of 500 mg/kg of alpha-methyldopa was found not only to induce mesenteric arteriolar vasodilatation gradually but also to depress arteriolar reponsiveness to catecholamines [18].
  • It is concluded that the high affinity, warm-reactive IgM and not the IgG antibodies are primarily responsible for clinically manifest anemia in patients receiving alphamethyldopa and that the hemolytic activity is probably mediated by the classic pathway of complement activation [19].
  • Flow cytometric data suggest that sensitivity of tumor cells to Aldomet is not related to the cell cycle [20].
  • This review outlines the mechanisms of adrenergic control of the circulation and how the proposed mechanisms of action of methyldopa (ie, dopa decarboxylation, false neurotransmission, inhibition of renin release, and stimulation of alpha receptor sites in the brain) seem to account for the depressor action of the drug [21].

Anatomical context of methyldopa


Associations of methyldopa with other chemical compounds


Gene context of methyldopa

  • Genetic reconstruction experiments in which Ddc+ and amd+ gene doses are varied show that increasing DDC activity does not lead to a measurable increase in resistance to dietary alpha-methyldopa [31].
  • This suggests that the increased resistance to dietary alpha-methyldopa is not the result of increased DDC activity but, rather, results from increased l(2)amd+ activity [31].
  • These experiments were performed to determine whether individual variations in red blood cell (RBC) COMT and platelet PST activities might reflect variations in the metabolism of methyldopa in man [32].
  • The thermolabile (TL) form of the enzyme phenol sulfotransferase (PST) catalyzes the sulfation of catecholamine neurotransmitters and drugs such as methyldopa and acetaminophen [33].
  • Effects of methyldopa on prolactin and growth hormone [34].

Analytical, diagnostic and therapeutic context of methyldopa

  • The type of treatment (diuretics alone or diuretics plus methyldopa) did not affect ECG voltages during the first year of follow-up [35].
  • To compare the antihypertensive efficacy of methyldopa administered once at bedtime with the same total dose given three times daily, a double-blind crossover study was performed in 14 patients previously well controlled on methyldopa [36].
  • A double blind study to evaluate the effect of methyldopa on menopausal vasomotor flushes [37].
  • Here too, prior administration of 5,7-DHT either intracerebroventricularly or directly into the cervical cord largely prevented the hypotensive action of the microinjections of methyldopa [38].
  • Inulin clearance fell by 13% (p less than 0.05), and filtration fraction fell from 0.23 to 0.18 (p less than 0.02), but other parameters of renal function did not change with methyldopa [39].


  1. The effects of antihypertensive therapy on the quality of life. Croog, S.H., Levine, S., Testa, M.A., Brown, B., Bulpitt, C.J., Jenkins, C.D., Klerman, G.L., Williams, G.H. N. Engl. J. Med. (1986) [Pubmed]
  2. Impaired reticuloendothelial function in patients treated with methyldopa. Kelton, J.G. N. Engl. J. Med. (1985) [Pubmed]
  3. Alpha-methyldopa and carotid-sinus hypersensitivity. Morley, C.A., Perrins, E.J., Sutton, R. N. Engl. J. Med. (1981) [Pubmed]
  4. Methyldopa inhibition of suppressor-lymphocyte function: a proposed cause of autoimmune hemolytic anemia. Kirtland, H.H., Mohler, D.N., Horwitz, D.A. N. Engl. J. Med. (1980) [Pubmed]
  5. Methyldopa-induced thrombocytopenia in chronic lymphocytic leukemia. Shalev, O., Brezis, M. N. Engl. J. Med. (1977) [Pubmed]
  6. alpha-Methyldopa and depression: a clinical study and review of the literature. DeMuth, G.W., Ackerman, S.H. The American journal of psychiatry. (1983) [Pubmed]
  7. Biochemical and dynamic responses to single and repeated doses of methyldopa and propranolol during dynamic physical activity. Rosenthal, L., Affrime, M.B., Lowenthal, D.T., Falkner, B., Saris, S., Gould, A.B. Clin. Pharmacol. Ther. (1982) [Pubmed]
  8. Effects of methyldopa on psychometric performance. Johnson, B., Hoch, K., Errichetti, A., Johnson, J. Journal of clinical pharmacology. (1990) [Pubmed]
  9. Neurobehavioral teratogenic effects of clomipramine and alpha-methyldopa. De Boer, S., Mirmiran, M., Van Haaren, F., Louwerse, A., van de Poll, N.E. Neurotoxicology and teratology. (1989) [Pubmed]
  10. Plasma concentration of alpha-methyldopa and sulphate conjugate after oral administration of methyldopa and intravenous administration of methyldopa and methyldopa hydrochloride ethyl ester. Saavedra, J.A., Reid, J.L., Jordan, W., Rawlins, M.D., Dollery, C.T. Eur. J. Clin. Pharmacol. (1975) [Pubmed]
  11. Acute colitis with methyldopa. Graham, C.F., Gallagher, K., Jones, J.K. N. Engl. J. Med. (1981) [Pubmed]
  12. Sinus node dysfunction caused by methyldopa and digoxin. Davis, J.C., Reiffel, J.A., Bigger, J.T. JAMA (1981) [Pubmed]
  13. Comparison of oxprenolol and methyldopa in hypertension. A within-patient double-blind trial. Barritt, D.W., Marshall, A.J., Heaton, S. Lancet (1976) [Pubmed]
  14. Short- and long-term efficacy of a calcium-antagonistic agent (nifedipine) combined with methyldopa in the treatment of severe hypertension. Guazzi, M.D., Fiorentini, C., Olivari, M.T., Bartorelli, A., Necchi, G., Polese, A. Circulation (1980) [Pubmed]
  15. Methyldopa-induced systemic lupus erythematosus. Nordstrom, D.M., West, S.G., Rubin, R.L. Arthritis Rheum. (1989) [Pubmed]
  16. The effect of single-dose methyldopa and diuretic on BP and left ventricular mass. Weinstein, M., Hilewitz, H., Rogel, S. Arch. Intern. Med. (1984) [Pubmed]
  17. Mortality and morbidity results from the European Working Party on High Blood Pressure in the Elderly trial. Amery, A., Birkenhäger, W., Brixko, P., Bulpitt, C., Clement, D., Deruyttere, M., De Schaepdryver, A., Dollery, C., Fagard, R., Forette, F. Lancet (1985) [Pubmed]
  18. Pharmacological effects of alpha-methyldopa, alpha-methylnorepinephrine, and octopamine on rat arteriolar, arterial, and terminal vascular smooth. Altura, B.M. Circ. Res. (1975) [Pubmed]
  19. Serologic profile of alphamethyldopa-induced hemolytic anemia: correlation between cell-bound IgM and hemolysis. Lalezari, P., Louie, J.E., Fadlallah, N. Blood (1982) [Pubmed]
  20. Toxicity of methyldopa (Aldomet) to mouse neuroblastoma cells in vivo. Chelmicka-Schorr, E., Sportiello, M.G., Otten, G.R., Arnason, B.G. Cancer Res. (1983) [Pubmed]
  21. Methyldopa. Mechanisms and treatment 25 years later. Frohlich, E.D. Arch. Intern. Med. (1980) [Pubmed]
  22. Diet and uptake of aldomet by the brain: competition with natural large neutral amino acids. Markovitz, D.C., Fernstrom, J.D. Science (1977) [Pubmed]
  23. Ultrastructural mapping of methyldopa and anti-D IgG erythrocyte antigen receptors. Masouredis, S.P., Sudora, E. J. Clin. Invest. (1975) [Pubmed]
  24. Cardiovascular regulation by central adrenergic mechanisms and its alteration by hypotensive drugs. Haeusler, G. Circ. Res. (1975) [Pubmed]
  25. Alpha-methyldopa disposition in mothers with hypertension and in their breast-fed infants. White, W.B., Andreoli, J.W., Cohn, R.D. Clin. Pharmacol. Ther. (1985) [Pubmed]
  26. Rauwolfia use and breast cancer: a case-control study. Stanford, J.L., Martin, E.J., Brinton, L.A., Hoover, R.N. J. Natl. Cancer Inst. (1986) [Pubmed]
  27. Effects of guanethidine and methyldopa on a standardized test for renin responsiveness. Lowder, S.C., Liddle, G.W. Ann. Intern. Med. (1975) [Pubmed]
  28. Letter: Alpha methyldopa and forgetfulness. Fernandez, P.G. Ann. Intern. Med. (1976) [Pubmed]
  29. Treatment of severe hypertension with labetalol compared with methyldopa and furosemide. Results of a long-term, double-blind, multicenter trial. Wallin, J.D., Wilson, D., Winer, N., Maronde, R.F., Michelson, E.L., Langford, H., Maloy, J., Poland, M. Am. J. Med. (1983) [Pubmed]
  30. Antihypertensive treatment and plasma lipoprotein levels. The associations in data from a population study. MacMahon, S.W., Macdonald, G.J. Am. J. Med. (1986) [Pubmed]
  31. Evidence for regulatory variants of the dopa decarboxylase and alpha-methyldopa hypersensitive loci in Drosophila. Marsh, J.L., Wright, T.R. Genetics (1986) [Pubmed]
  32. Platelet phenol sulfotransferase and erythrocyte catechol-O-methyltransferase activities: correlation with methyldopa metabolism. Campbell, N.R., Dunnette, J.H., Mwaluko, G., Van Loon, J., Weinshilboum, R.M. Clin. Pharmacol. Ther. (1984) [Pubmed]
  33. Inheritance of human platelet thermolabile phenol sulfotransferase (TL PST) activity. Price, R.A., Cox, N.J., Spielman, R.S., Van Loon, J.A., Maidak, B.L., Weinshilboum, R.M. Genet. Epidemiol. (1988) [Pubmed]
  34. Effects of methyldopa on prolactin and growth hormone. Steiner, J., Cassar, J., Mashiter, K., Dawes, I., Fraser, T.R., Breckenridge, A. British medical journal. (1976) [Pubmed]
  35. Left ventricular hypertrophy in elderly hypertensive patients: a report from the European Working Party on High Blood Pressure in the Elderly trial. Van Hoof, R. Am. J. Med. (1991) [Pubmed]
  36. Antihypertensive efficacy of a single bedtime dose of methyldopa. Wright, J.M., McLeod, P.J., McCullough, W. Clin. Pharmacol. Ther. (1976) [Pubmed]
  37. A double blind study to evaluate the effect of methyldopa on menopausal vasomotor flushes. Hammond, M.G., Hatley, L., Talbert, L.M. J. Clin. Endocrinol. Metab. (1984) [Pubmed]
  38. Bulbospinal serotonin pressor pathways and hypotensive action of methyldopa in the rat. Chalmers, J.P., Minson, J.B., Choy, V. Hypertension (1984) [Pubmed]
  39. Effects of labetalol and methyldopa on renal function. Cruz, F., O'Neill, W.M., Clifton, G., Wallin, J.D. Clin. Pharmacol. Ther. (1981) [Pubmed]
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