AbstractThe enantiomers of 1‐methyl‐3‐(10H‐phenothiazine‐10‐ylmethyl)‐1‐azoniabicyclo[2,2,2]octane iodide (1) were prepared by chiral chromatographic resolution of the precursor mequitazine (2). The (+)‐(S)‐enantiomer 1b is 10‐fold more potent than (−)‐(R)‐enantiomer 1a as a histamine antagonist, while the two enantiomers show the same antimuscarinic activity in vitro. The absolute configuration of the more active dextrorotatory isomer has been determined by X‐ray analysis. Conformational analysis and molecular modeling suggest that the (+)‐(S)‐enantiomer can adopt a conformation similar to that attributed to the receptor binding conformers of classical antihistamines. © 1994 Wiley‐Liss, Inc.

01 Jun 1992·Pulmonary Pharmacology

Effect of mequitamium iodide (LG 30435) on airway microvascular leakage in the guinea-pig

Article

Author: Nappi, F. ; Subissi, A. ; Manzini, S. ; Giachetti, A. ; Abelli, L.

Intravenous administration of mequitamium iodide (LG 30435) prevented the increase of tracheobronchial vascular permeability induced either by antigen challenge or by exogenous histamine in the guinea-pig, while it was ineffective against PAF, serotonin or capsaicin. These findings indicate that mequitamium iodide selectively interferes with the effect of histamine on airway microvascular leakage, mediated by histamine H1 receptors, and is more potent than diphenhydramine, mequitazine or astemizole. Histamine receptor antagonism is likely to be major determinant of the antiallergic activity of the compound, although additional mechanisms may be involved.

01 Jul 1990·European Journal of PharmacologyQ3 · MEDICINE

High-affinity binding of mequitamium iodide (LG 30435) to muscarinic and histamine H1 receptors

Q3 · MEDICINE

Article

Author: Renzetti, Anna R. ; Barone, Domenico ; Criscuoli, Marco

Mequitamium iodide (LG 30435) is a novel quaternary ammonium phenothiazine with potential as an anti-asthmatic agent. In vitro binding experiments were performed in order to clarify the molecular mechanisms underlying its biological activity. Mequitamium iodide was found to bind with high affinity only to histamine H1 receptors in rat brain membranes (Ki = 9 nM) and to muscarinic acetylcholine receptors in various tissues homogenates (Ki = 12-77 nM) with no clearcut selectivity for any of the known subtypes. The interaction with muscarinic receptors in rat cerebral cortex and lung parenchyma was competitive, as showed by saturation studies. Lower affinity values (Ki = 1-10 microM) were found for serotonin 5-HT2, platelet-activating factor (PAF), verapamil and beta-adrenergic agents. These results indicate that both the potent antimuscarinic and antihistamine and the relatively weak anti-PAF pharmacological effects of mequitamium iodide may be explained by the direct interaction of the substance with the respective receptors.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	-	-	-
Asthma	Phase 2	FR	-	-
Asthma	Phase 2	-	Laboratori Guidotti SpA	-
Asthma	Phase 2	IT	Guidotti SRL	-
Rhinitis	Phase 2	IT	Guidotti SRL	-
Rhinitis	Phase 2	FR	-	-
Rhinitis	Phase 2	-	-	-

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