histamine H4 receptor; HH4R; G-protein coupled receptor 105; GPRv53; SP9144; AXOR35; Pfi-013 (HRH4, GPCR105)

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Function

Structure

belongs to the G-protein coupled receptor 1 family

Compartment

cell membrane

Expression

Pharmacology

  • does not bind diphenhydramine, loratadine, ranitidine, cimetidine or chlorpheniramine
  • shows shows modest affinity for dimaprit, impromidine, clobenpropit, thioperamide, burimamide clozapine, immepip & imetit
  • the order of inhibitory activity is imetit > clobenpropit > burimamide > thioperamide
  • clobenpropit behaves as a partial agonist
  • dimaprit & impromidine show some agonist activity
  • clozapine behaves as a full agonist
  • thioperamide shows inverse agonism (enhances cAMP activity)
  • the order of inhibitory activity of histamine derivatives was histamine > N-alpha-methylhistamine > R(-)-alpha- methylhistamine > S(+)-alpha-methylhistamine
  • both N-alpha-methylhistamine > R(-)-alpha-methylhistamine behave as full agonists

More general terms

Additional terms

References

Database