Abstract
1 A series of cationic, lipophilic histamine H1-receptor antagonists, neuroleptics, antidepressants and monoamine oxidase inhibitors were tested for their effects on anti-IgE-induced histamine release from human lung fragments in vitro. 2 They had a biphasic effect: at low concentrations a dose-related inhibition of histamine release was observed whereas, at higher concentrations, the drugs liberated histamine even in the absence of antigen. 3 Mepyramine, a much less lipophilic drug than the others tested, was only weakly active on mast cells at pharmacological concentrations. 4 The potency of the drugs as release inhibitors was not related quantitatively to their histamine liberating potency. 5 There was no; correlation between activity on mast cells and histamine H1-receptor antagonism. 6 Mast cell stabilization may play a part in the activity of these drugs as anti-allergic agents.
MeSH Terms
Chlorpheniramine/pharmacology
Histamine H1 Antagonists/pharmacology
Histamine Release/drug effects
Humans
Immunoglobulin E/immunology
Lung/drug effects,metabolism
Mast Cells/drug effects
Pyrilamine/pharmacology
Chemicals
Histamine H1 Antagonists
Immunoglobulin E
Chlorpheniramine
Pyrilamine
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Church M K
Gradidge C F
References (26)
26 references, click to expand
-
Histamine release by antihistamines.
J Physiol. 1953 Mar;119(4):47P-48P
PMID: 13053466
-
Clinical investigation of agents with prophylactic anti-allergic effects in bronchial asthma.
Clin Allergy. 1978 Jul;8(4):373-82
PMID: 101313
-
The role of the alkaline earth ions in anaphylactic histamine secretion.
J Physiol. 1972 Aug;224(3):753-69
PMID: 4116105
-
The protective effect of ketotifen in bronchial asthma.
J Int Med Res. 1978;6(2):78-85
PMID: 24563
-
Interaction of antihistamines with lipid bilayers.
Biochem Pharmacol. 1979 Jul 15;28(14):2199-205
PMID: 40556
-
Exercise-induced bronchoconstriction in patients with bronchial asthma. Its prevention with an antihistaminic agent.
Respiration. 1977;34(1):31-5
PMID: 16323
-
Some quantitative uses of drug antagonists.
Br J Pharmacol Chemother. 1959 Mar;14(1):48-58
PMID: 13651579
-
Inhibition of histamine release and ionophore-induced calcium flux in rat mast cells by lidocaine and chlorpromazine.
Agents Actions. 1979 Aug;9(3):239-43
PMID: 91313
-
The relationship between the lipophilic nature of tricyclic neuroleptics and antidepressants, and histamine release.
Eur J Pharmacol. 1972 May;18(2):139-47
PMID: 4113999
-
Bronchodilating activity of an H1 blocker, chlorpheniramine.
J Allergy Clin Immunol. 1977 Jan;59(1):54-63
PMID: 13094
-
The action of local anaesthetics on histamine release.
Biochem Pharmacol. 1976 Aug 1;25(15):1747-50
PMID: 60105
-
Amitriptyline and asthma.
Med J Aust. 1971 Jul 3;2(1):25-8
PMID: 4937682
-
Clinical experience with amitriptyline (tryptanol) in the treatment of bronchial asthma.
Ann Allergy. 1965 Sep;23(9):422-9
PMID: 5830238
-
The pharmacological properties of a new, orally active antianaphylactic compound: ketotifen, a benzocycloheptathiophene.
Arzneimittelforschung. 1978;28(5):770-82
PMID: 35171
-
Protection tests on bronchial allergen challenge with disodium cromoglycate and thiazinamium.
J Allergy. 1970 Jul;46(1):1-11
PMID: 4393190
-
The anti-anaphylactic and histamine-releasing properties of the antihistamines. Their effect on the mast cells.
Br J Pharmacol Chemother. 1960 Sep;15:396-404
PMID: 13773171
-
Drug antagonism and pAx.
Pharmacol Rev. 1957 Jun;9(2):242-6
PMID: 13465304
-
An automated fluorimetric assay for the rapid determination of histamine in biological fluids.
Life Sci II. 1973 Apr 8;12(7):327-36
PMID: 4121709
-
Double-blind placebo-controlled clinical evaluation of oxatimide (R 35443). A novel potent anti-allergic drug in the treatment of hay fever.
Acta Allergol. 1977 Aug;32(4):278-89
PMID: 70947
-
Oxatomide protects Trichinella spiralis infected mice from lethal anaphylaxis.
Agents Actions. 1978 Dec;8(6):568-71
PMID: 742554
-
Bronchodilatation after inhalation of the antihistamine clemastine.
Thorax. 1978 Aug;33(4):479-82
PMID: 694800
-
Morphological evaluation of oxatomide--a new anti-allergic drug in guinea pig anaphylaxis.
Int Arch Allergy Appl Immunol. 1978;56(6):507-16
PMID: 24593
-
On the mechanism of chlorpromazine-induced histamine release from rat mast cells.
Acta Physiol Scand. 1971 Nov;83(3):412-21
PMID: 4109134
-
The membrane actions of anesthetics and tranquilizers.
Pharmacol Rev. 1972 Dec;24(4):583-655
PMID: 4565956
-
Anti-asthmatic properties of a new peroral drug (HC 20-5II).
Acta Allergol. 1977 Feb;32(1):27-34
PMID: 320807
-
The effects of the H1 and H2 antihistamines on "allergic" histamine release and its inhibition by histamine.
J Pharmacol Exp Ther. 1975 Feb;192(2):441-50
PMID: 46921