TY - JOUR
T1 - Tricyclic antidepressants
T2 - Potent blockade of histamine H1 receptors of guinea pig ileum
AU - Figge, James
AU - Leonard, Paul
AU - Richelson, Elliott
N1 - Funding Information:
Supported by Mayo Foundation and USPHS GrantsD A 1490 and MH 27692.W e thank Dr. F.G. Prendergasfto r critical review of this manuscript; Dr. J. Szurszewskfio r the use of his computer facilities; P. Schmalzf or the computepr rogramminagn;d the following companies for drugs: CIBA-Geigy, Lilly, Merck Sharp and Dohme, Smith Kline and French, and USV Pharmaceutical.
PY - 1979/10/15
Y1 - 1979/10/15
N2 - Six tricyclic antidepressants were tested for their ability to antagonize histamine actions at histamine H1 receptors in a bioassay for these receptors (histamine-induced contractions of guinea pig ileum). All compounds were competitive antagonists with equilibrium dissociation constants in the range of 5.6 x 10-11 M to 1.5 x 10-7 M. Doxepin hydrochloride and amitriptyline hydrochloride were the most potent compounds of the series and may be the most potent antihistamines known. Antagonism at histamine H1 receptors by these compounds may explain their sedative effects.
AB - Six tricyclic antidepressants were tested for their ability to antagonize histamine actions at histamine H1 receptors in a bioassay for these receptors (histamine-induced contractions of guinea pig ileum). All compounds were competitive antagonists with equilibrium dissociation constants in the range of 5.6 x 10-11 M to 1.5 x 10-7 M. Doxepin hydrochloride and amitriptyline hydrochloride were the most potent compounds of the series and may be the most potent antihistamines known. Antagonism at histamine H1 receptors by these compounds may explain their sedative effects.
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U2 - 10.1016/0014-2999(79)90320-0
DO - 10.1016/0014-2999(79)90320-0
M3 - Article
C2 - 41726
AN - SCOPUS:0018605003
SN - 0014-2999
VL - 58
SP - 479
EP - 483
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 4
ER -