Date published: 2026-5-9

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Immethridine dihydrobromide (CAS 87976-03-2)

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Alternate Names:
4-(1H-Imidazol-4-ylmethyl)pyridine dihydrobromide
Application:
Immethridine dihydrobromide is a strong and highly selective histamine H3 receptor agonist
CAS Number:
87976-03-2
Molecular Weight:
321.01
Molecular Formula:
C9H9N32HBr
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Immethridine dihydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively). Immethridine dihydrobromide does not bind to H1 or H2 receptors at concentrations up to 10 μM.


Immethridine dihydrobromide (CAS 87976-03-2) References

  1. Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.  |  Kitbunnadaj, R., et al. 2004. J Med Chem. 47: 2414-7. PMID: 15115383
  2. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.  |  Lim, HD., et al. 2005. J Pharmacol Exp Ther. 314: 1310-21. PMID: 15947036
  3. Histamine H(3) receptors are involved in the protective effect of ghrelin against HCl-induced gastric damage in rats.  |  Adami, M., et al. 2010. Pharmacology. 86: 259-66. PMID: 20975320
  4. NAADP links histamine H1 receptors to secretion of von Willebrand factor in human endothelial cells.  |  Esposito, B., et al. 2011. Blood. 117: 4968-77. PMID: 21364192
  5. Histamine H1, H3 and H4 receptors are involved in pruritus.  |  Rossbach, K., et al. 2011. Neuroscience. 190: 89-102. PMID: 21689731
  6. Selective histamine H₃ and H₄ receptor agonists exert opposite effects against the gastric lesions induced by HCl in the rat stomach.  |  Coruzzi, G., et al. 2011. Eur J Pharmacol. 669: 121-7. PMID: 21839070
  7. Luciferase reporter gene assay on human, murine and rat histamine H4 receptor orthologs: correlations and discrepancies between distal and proximal readouts.  |  Nordemann, U., et al. 2013. PLoS One. 8: e73961. PMID: 24023919
  8. Involvement of histaminergic inputs in the jaw-closing reflex arc.  |  Gemba, C., et al. 2015. J Neurophysiol. 113: 3720-35. PMID: 25904711
  9. Histamine Stimulates Ciliary Beat Frequency via the H2 Receptor in the Protochordate Botryllus schlosseri.  |  Cima, F. and Franchi, N. 2016. J Exp Zool B Mol Dev Evol. 326: 176-92. PMID: 27139577
  10. Immethridine, histamine H3-receptor (H3R) agonist, alleviated experimental autoimmune encephalomyelitis via inhibiting the function of dendritic cells.  |  Shi, Y., et al. 2017. Oncotarget. 8: 75038-75049. PMID: 29088843
  11. Histamine elicits glutamate release from cultured astrocytes.  |  Kárpáti, A., et al. 2018. J Pharmacol Sci. 137: 122-128. PMID: 29858014
  12. Activation of orexinergic and histaminergic pathway involved in therapeutic effect of histamine H4 receptor antagonist against cisplatin-induced anorexia in mice.  |  Yamamoto, K., et al. 2019. Naunyn Schmiedebergs Arch Pharmacol. 392: 925-936. PMID: 30919010
  13. Histamine receptor agonist alleviates severe cardiorenal damages by eliciting anti-inflammatory programming.  |  Noguchi, K., et al. 2020. Proc Natl Acad Sci U S A. 117: 3150-3156. PMID: 31992639
  14. Histamine depolarizes rat intracardiac ganglion neurons through the activation of TRPC non-selective cation channels.  |  Sato, A., et al. 2020. Eur J Pharmacol. 886: 173536. PMID: 32896550
  15. Histamine H3 receptor antagonism modulates autism-like hyperactivity but not repetitive behaviors in BTBR T+Itpr3tf/J inbred mice.  |  Molenhuis, RT., et al. 2022. Pharmacol Biochem Behav. 212: 173304. PMID: 34856309

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Immethridine dihydrobromide, 10 mg

sc-203603
10 mg
$151.00

Immethridine dihydrobromide, 50 mg

sc-203603A
50 mg
$640.00