The pharmacology and mechanisms of action of histamine H<sub>1</sub>‐antagonists

Rimmer, S. J.; Church, Martin K.

doi:10.1111/j.1365-2222.1990.tb02456.x

Cited by 77 publications

(48 citation statements)

References 132 publications

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“…These compounds produce the inhibition of the e¡ects of histamine mediated by H 1 receptors such as smooth-muscle contraction in the respiratory and gastrointestinal tracts, pruritus, sneezing by sensory-nerve stimulation, vasodilation (Simons and Simons, 1994). Therefore, their most common use is in the treatment of allergic disorders (Rimer and Church, 1990). In addition to these wellknown peripheral e¡ects, H 1 -receptor antagonists produce various central inhibitory actions (Simons and Simons, 1994).…”

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confidence: 99%

“…H 1 -antagonists are also able to potentiate opioid analgesia in laboratory animals (Sun et al, 1985;Yeh, 1985;Malec, 1987). It has also been observed that some antihistamines, such as hydroxyzine, diphenhydramine, pyrilamine and promethazine, are endowed with analgesic properties in both laboratory animals (Stambaugh and Lane, 1983;Rumore and Schlichting, 1985;Sun et al, 1985;Rumore and Schlichting, 1986) and humans (Campos and Solis, 1980;Rumore and Schlichting, 1986).…”

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confidence: 99%

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Antihistamine antinociception is mediated by Gi-protein activation

Galeotti¹,

Ghelardini²,

Bartolini³

2002

Neuroscience

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AbstractöThe e¡ect of the i.c.v. administration of antisense oligodeoxynucleotides directed against the K subunit of di¡erent Gi-proteins (anti-GiK 1 , anti-GiK 2 , anti-GiK 3 ) on the antinociception induced by the H 1 -antihistamines was evaluated in the mouse hot-plate test. The administration of diphenhydramine (20 mg kg 31 s.c.), pyrilamine (15 mg kg 31 s.c.) and promethazine (6 mg kg 31 s.c.) produced an increase of the pain threshold which peaked 15 min after injection. Pretreatment with anti-GiK 1 (12.5 Wg per mouse i.c.v.), anti-GiK 2 (25 Wg per mouse i.c.v.) and anti-GiK 3 (25 Wg per mouse i.c.v.), administered 24 and 18 h before test, prevented the antihistamine-induced antinociception. At the highest e¡ective doses, none of the compounds used impaired motor coordination, as revealed by the rota rod test, nor modi¢ed spontaneous motility and inspection activity, as revealed by the hole board test.These results suggest an important role played by the Gi-protein pathway in the transduction mechanism involved in the enhancement of the pain threshold produced by H 1 -antihistamines. ß

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confidence: 99%

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confidence: 99%

Antihistamine antinociception is mediated by Gi-protein activation

Galeotti¹,

Ghelardini²,

Bartolini³

2002

Neuroscience

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“…Experimental allergic rhinitis has usually been induced by intranasal application of antigen in sensi tized animals, resulting in an increased nasal vascular permeability and intranasal resistance (16,20,21). In spite of the increasing evidence of the role of several other mediators (22,23), histamine is still regarded as the prin cipal mediator of antigen-induced allergic skin reactions and rhinitis. In addition, intradermal and intranasal appli cation of chemical mediators and chemical mediator re leasers increase vascular permeability in a manner similar to that of allergic models (12,14).…”

Section: Discussionmentioning

confidence: 99%

Antiallergic Effects of ZCR-2060: Effect on Allergic Cutaneous Reactions and Rhinitis Models in Mice and Rats

Omata

Yoshida

et al. 1994

Japanese Journal of Pharmacology

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ABSTRACT-The antiallergic action of 2-[2-[4-(diphenylmethyl)-1-piperadinyl]ethoxy]benzoic acid maleate (ZCR-2060) was investigated on allergic cutaneous reactions and nasal vascular permeability in mice and rats. ZCR-2060 markedly inhibited immediate allergic cutaneous reactions, including passive cutaneous anaphylaxis (PCA) in rats and mice; histamine-, compound 48/80 and calcium ionophore A 23187-induced cutaneous reactions in rats; and biphasic skin reactions mediated by monoclonal IgE anti body and epicutaneous challenge with antigen in mice, but did not affect 5-hydroxytryptamine-induced cutaneous reaction in rats. The antigen-induced nasal vascular permeability increase in actively and passive ly sensitized rats and histamine-induced nasal vascular permeability increase in rats (allergic rhinitis model) were clearly inhibited in a dose-dependent fashion by ZCR-2060. Moreover, ZCR-2060 significantly inhib ited antigen-induced anaphylactic histamine release from rat peritoneal mast cells and carrageenin-induced paw edema in rats. These results suggest that ZCR-2060 has antiallergic effects on allergic cutaneous reac tions and experimental rhinitis, probably due to histamine H,-receptor blockage and the inhibition of histamine release.

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“…These adverse effects have severely limited the use of this medication. The newer H,-receptor antagonists display high affinity for the H,-receptor with fewer effects on the other receptors and produce no CNS effect (8). However, ketotifen and terfenadine at high doses have an affinity for cholinergic and 5-HT receptors.…”

Section: Effect On Thiopental-induced Sleep In Micementioning

confidence: 99%

“…Since then, many histamine H,-receptor antagonists have been developed. Classical histamine H,-receptor an tagonists such as mepyramine, chlorphenilamine and diphenhydramine have been widely used for the treatment of allergic rhinitis and skin diseases (8). However, these drugs readily cross the blood-brain barrier and have the capacity to cause symptoms of central nervous system (CNS) depression such as sedation.…”

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Antiallergic Effect of ZCR-2060: Antihistaminic Action

Omata

Yoshida

et al. 1994

Japanese Journal of Pharmacology

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ABSTRACT-The antihistaminic effect of 2-[2-[4-(diphenylmethyl)-1-piperadinyl]ethoxy]benzoic acid maleate (ZCR-2060), a newly synthesized antiallergic agent, was investigated in both in vitro and in vivo studies. ZCR-2060 clearly antagonized histamine-induced contraction of isolated guinea pig ileum and trachea. In contrast, carbachol-, BaC12 and 5-hydroxytryptamine-induced contractions of isolated guinea pig ileum were slightly inhibited by higher concentrations of ZCR-2060. 3H-Mepyramine specific binding to membranes from guinea pig lung and brain were markedly inhibited by ZCR-2060 in a concentration-de pendent fashion. In the in vitro studies, the antihistaminic effect of ZCR-2060 was greater than those of cetirizine and terfenadine, but was less than that of ketotifen. In the in vivo studies, ZCR-2060 significantly inhibited the histamine-induced cutaneous reaction in rats, when administered orally 1 hr before the histamine injection. Moreover, ZCR-2060 has a long-lasting antihistaminic effect. In the in vivo studies, the antihistaminic effect of ZCR-2060 was found to be greater than that of cetirizine and terfenadine, and it was the same as that of ketotifen. Thiopental-induced sleep and spontaneous ambulatory activity in mice, however, were unaffected by ZCR-2060 at higher doses. These results indicate that ZCR-2060 has a potent, selective and long acting histamine H,-receptor antagonistic action without causing any unwanted CNS side effect.

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The pharmacology and mechanisms of action of histamine H₁‐antagonists

Cited by 77 publications

References 132 publications

Antihistamine antinociception is mediated by Gi-protein activation

Antihistamine antinociception is mediated by Gi-protein activation

Antiallergic Effects of ZCR-2060: Effect on Allergic Cutaneous Reactions and Rhinitis Models in Mice and Rats

Antiallergic Effect of ZCR-2060: Antihistaminic Action

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The pharmacology and mechanisms of action of histamine H1‐antagonists

Cited by 77 publications

References 132 publications

Antihistamine antinociception is mediated by Gi-protein activation

Antihistamine antinociception is mediated by Gi-protein activation

Antiallergic Effects of ZCR-2060: Effect on Allergic Cutaneous Reactions and Rhinitis Models in Mice and Rats

Antiallergic Effect of ZCR-2060: Antihistaminic Action

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The pharmacology and mechanisms of action of histamine H₁‐antagonists