Characterization of functional histamine H1 receptors on a cultured smooth muscle cell line

J Cell Physiol. 1988 Mar;134(3):367-75. doi: 10.1002/jcp.1041340307.


Cultured cells of the smooth muscle line DDT1MF-2, which was derived from a hamster vas deferens tumor, expressed histamine H1-type receptors and responded biochemically and functionally to H1-specific stimulation. The H1-receptor antagonist [3H]-pyrilamine bound specifically to 9.7 x 10(6) sites/DDT1MF-2 cell with a dissociation constant (Kd) of 219 nM. The addition of histamine to suspensions of fura-2-loaded DDT1MF-2 cells elicited a rapid, transient, and stimulus concentration-dependent increase in the intracellular concentration of Ca2+ with an EC50 of 3 x 10(-5) M, which demonstrated H1 receptor specificity. Moreover, in order to evaluate in vitro contractile response of individual DDT1MF-2 cells, the degree of intracellular actin polymerization was quantified by a DNase inhibition assay. The percentage of nonpolymerized or G-actin in DDT1MF-2 cells was reduced in a histamine concentration-dependent manner with an EC50 of 1 x 10(-5) M and H1 receptor specificity. Histamine-induced actin polymerization was accompanied by changes in cell shape that were consistent with cellular contraction, as assessed by flow cytometry. The H1-type receptors of cultured DDT1MF-2 cells thus couple histamine stimulation to a variety of functional responses of smooth muscle cells.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Actins / metabolism
  • Animals
  • Calcium / metabolism
  • Cell Line
  • Cricetinae
  • Deoxyribonucleases / antagonists & inhibitors
  • Flow Cytometry
  • Histamine / metabolism*
  • Histamine / pharmacology
  • Ligands
  • Male
  • Muscle Contraction
  • Muscle, Smooth / metabolism*
  • Polymers
  • Pyrilamine / metabolism
  • Receptors, Histamine / analysis*
  • Receptors, Histamine H1 / analysis*
  • Receptors, Histamine H1 / metabolism
  • Software
  • Vas Deferens / metabolism


  • Actins
  • Ligands
  • Polymers
  • Receptors, Histamine
  • Receptors, Histamine H1
  • Histamine
  • Deoxyribonucleases
  • Pyrilamine
  • Calcium