Date published: 2026-5-1

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Metoprine (CAS 7761-45-7)

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Alternate Names:
5-(3,4-Dichlorophenyl)-6-methyl-2,4-pyrimidinediamine
Application:
Metoprine is a 2,4-Diaminopyrimidine derivative as antimalarial agent.
CAS Number:
7761-45-7
Purity:
≥97%
Molecular Weight:
269.13
Molecular Formula:
C11H10Cl2N4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Metoprine functions as a histone methyltransferase inhibitor. It acts by inhibiting the enzyme histone methyltransferase, which is responsible for adding methyl groups to histone proteins. By inhibiting this enzyme, Metoprine disrupts the process of histone methylation, which plays a role in regulating gene expression and chromatin structure. This disruption can lead to alterations in gene transcription and ultimately impact cellular processes. Metoprine′s mechanism of action involves interfering with the epigenetic regulation of gene expression at the molecular level, making it useful for studying the role of histone methylation in various biological processes.


Metoprine (CAS 7761-45-7) References

  1. Metoprine-induced thirst and diuresis in Wistar rats.  |  Lecklin, A., et al. 1999. Acta Physiol Scand. 165: 325-33. PMID: 10192183
  2. Antiamnesic effect of metoprine and of selective histamine H(1) receptor agonists in a modified mouse passive avoidance test.  |  Malmberg-Aiello, P., et al. 2000. Neurosci Lett. 288: 1-4. PMID: 10869801
  3. Cardiac and regional haemodynamic effects of histamine N-methyltransferase inhibitor metoprine in haemorrhage-shocked rats.  |  Jochem, J. 2004. Inflamm Res. 53: 316-23. PMID: 15241567
  4. Effects of (S)-alpha -fluoromethylhistidine and metoprine on locomotor activity and brain histamine content in mice.  |  Sakai, N., et al. 1992. Life Sci. 51: 397-405. PMID: 1635419
  5. Blockade of brain histamine metabolism alters methamphetamine-induced expression pattern of stereotypy in mice via histamine H1 receptors.  |  Kitanaka, J., et al. 2007. Neuroscience. 147: 765-77. PMID: 17570600
  6. Metoprine induced behavioral modifications and brain regional histamine increase in WAG/Rij and Wistar rats.  |  Samotaeva, IS., et al. 2012. Epilepsy Res. 101: 148-56. PMID: 22503455
  7. Lipid-soluble inhibitors of dihydrofolate reductase. I. Kinetics, tissue distribution, and extent of metabolism of pyrimethamine, metoprine, and etoprine in the rat, dog, and man.  |  Cavallito, JC., et al. 1978. Drug Metab Dispos. 6: 329-37. PMID: 26555
  8. Synergistic growth inhibition of rat hepatoma cells exposed in vitro to N10-propargyl-5,8-dideazafolate with methotrexate or the lipophilic antifolates trimetrexate or metoprine.  |  Galivan, J., et al. 1987. Cancer Res. 47: 5256-60. PMID: 2958130
  9. Metoprine, a histamine N-methyltransferase inhibitor, attenuates methamphetamine-induced hyperlocomotion via activation of histaminergic neurotransmission in mice.  |  Kitanaka, N., et al. 2021. Pharmacol Biochem Behav. 209: 173257. PMID: 34418452
  10. Changes in the rat brain histamine content following metoprine and other histamine-methyltransferase (HMT) inhibitors.  |  Zawilska, J. and Nowak, JZ. 1985. Pol J Pharmacol Pharm. 37: 821-30. PMID: 3832018
  11. Inhibition of brain histamine metabolism by metoprine.  |  Hough, LB., et al. 1986. Biochem Pharmacol. 35: 307-10. PMID: 3942601
  12. Biochemical correlates of responsiveness and collateral sensitivity of some methotrexate-resistant murine tumors to the lipophilic antifolate, metoprine.  |  Sirotnak, FM., et al. 1982. Cancer Res. 42: 924-8. PMID: 7059991
  13. Kinetics of metoprine, a lipid-soluble antifolate.  |  Jones, BR., et al. 1981. Br J Clin Pharmacol. 12: 675-80. PMID: 7332733
  14. Metoprine, an inhibitor of histamine N-methyltransferase but not catechol-O-methyltransferase, suppresses feeding in sated and in food deprived rats.  |  Lecklin, A., et al. 1995. Methods Find Exp Clin Pharmacol. 17: 47-52. PMID: 7542717
  15. The effect of metoprine on glucoprivic feeding induced by 2-deoxy-D-glucose.  |  Lecklin, A., et al. 1994. Pharmacol Biochem Behav. 49: 853-7. PMID: 7886098

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Metoprine, 25 mg

sc-484327
25 mg
$359.00