Sensory responses of human skin to synthetic histamine analogues and histamine

Br J Clin Pharmacol. 1980 May;9(5):461-5.


The potential for itch production in human skin of the synthetic analogues of histamine, 2-methyl histamine (an H1-receptor agonist) and 4-methyl histamine and dimaprit (H2-receptor agonists) has been studied in vivo and compared with histamine. Itch thresholds for 2-methyl histamine were consistently much higher than for histamine (P < 0.001). The H1-receptor antagonist chlorpheniramine raised the itch thresholds to 2-methyl histamine and histamine significantly (P < 0.001). Pruritus was not obtained with either 4-methyl histamine or dimaprit. No evidence of synergism between 2-methyl histamine and either 4-methyl histamine or dimaprit was found. The results suggest that histamine-induced pruritus is mediated in part through the H1-receptor and in part via an additional (but probably non-H2) mechanism.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Chlorpheniramine / pharmacology
  • Dimaprit
  • Female
  • Histamine / adverse effects*
  • Humans
  • Male
  • Methylhistamines / adverse effects*
  • Pruritus / chemically induced*
  • Pruritus / etiology
  • Receptors, Histamine H1 / physiology
  • Receptors, Histamine H2 / physiology
  • Skin / drug effects
  • Skin / metabolism
  • Thiourea / adverse effects*


  • Methylhistamines
  • Receptors, Histamine H1
  • Receptors, Histamine H2
  • Chlorpheniramine
  • 4-methylhistamine
  • Histamine
  • Thiourea
  • 2-methylhistamine
  • Dimaprit