A theoretical investigation of histamine tautomerism

J Med Chem. 1984 Nov;27(11):1531-4. doi: 10.1021/jm00377a023.

Abstract

Geometry optimizations of the structures of histamine (neutral and monocation) in the N(3)-H and N(1)-H tautomeric forms were performed at the ab initio Hartree-Fock level with the STO-3G basis set. Values of the structural parameters and their changes upon protonation and/or tautomerization are in good agreement with data from X-ray crystal-structure analysis of histamine and several analogues. Earlier predictions of the tautomeric preference from calculations using frozen geometries based on crystal-structure data are confirmed by calculations of energies of histamine in the fully optimized geometries with both the STO-3G and LP-3G basis sets and by comparisons of the minima in the molecular electrostatic potentials of the two tautomers. These results support a previously proposed model for the activation of the histamine H2 receptor.

Publication types

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

MeSH terms

  • Histamine*
  • Models, Chemical*
  • Stereoisomerism
  • X-Ray Diffraction

Substances

  • Histamine