Histamine Receptors and Antihistamines: From Discovery to Clinical Applications

Cataldi, Mauro; Borriello, Francesco; Granata, Francescopaolo; Annunziato, Lucio; Marone, Gianni

doi:10.1159/000358740

Cited by 45 publications

(35 citation statements)

References 126 publications

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“…H1R and H2R were widely expressed in a variety of tissues and immune cells, H3R has been confirmed to mainly localize in the brain, and H4R is preferentially expressed on immune cells, including mast cells [33]. Our results show that the three histamine receptors of H1R, H2R, and H4R were expressed in pterygium.…”

Section: Discussionsupporting

confidence: 52%

Proliferative Effects of Histamine on Primary Human Pterygium Fibroblasts

Qin

Zhang

et al. 2016

Mediators of Inflammation

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Purpose. It has been confirmed that inflammatory cytokines are involved in the progression of pterygium. Histamine can enhance proliferation and migration of many cells. Therefore, we intend to investigate the proliferative and migratory effects of histamine on primary culture of human pterygium fibroblasts (HPFs). Methods. Pterygium and conjunctiva samples were obtained from surgery, and toluidine blue staining was used to identify mast cells. 3-[4, 5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) was performed to evaluate the proliferative rate of HPFs and human conjunctival fibroblasts (HCFs); ki67 expression was also measured by immunofluorescence analysis. Histamine receptor-1 (H1R) antagonist (Diphenhydramine Hydrochloride) and histamine receptor-2 (H2R) antagonist (Nizatidine) were added to figure out which receptor was involved. Wound healing model was used to evaluate the migratory ability of HPFs. Results. The numbers of total mast cells and degranulated mast cells were both higher in pterygium than in conjunctiva. Histamine had a proliferative effect on both HPFs and HCFs, the effective concentration (10 μmol/L) on HPFs was lower than on HCFs (100 μmol/L), and the effect could be blocked by H1R antagonist. Histamine showed no migratory effect on HPFs. Conclusion. Histamine may play an important role in the proliferation of HPFs and act through H1R.

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Section: Discussionsupporting

confidence: 52%

Proliferative Effects of Histamine on Primary Human Pterygium Fibroblasts

Qin

Zhang

et al. 2016

Mediators of Inflammation

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“…Here, we also demonstrated that intrathecal doxylamine (11.65 μmol/kg) and triprolidine (4.66 μmol/kg) elicited spinal motor and sensory (proprioception and nociception) blockades. Our results resembled to the previous study that doxylamine (18 μmol; 80 μmol/kg) elicited completely cutaneous nociceptive block . In other words, the lower dose of intrathecal doxylamine than subcutaneous doxylamine to achieve the local anaesthetic effects.…”

Section: Discussionsupporting

confidence: 91%

“…Doxylamine, an antihistamine drug, is commonly used to relieve the symptoms of hay fever, atopic dermatitis, allergic rhinitis [1][2][3] and insomnia. [4] Triprolidine, an over-thecounter antihistamine, [5] was used in the treatment of skin irritation and allergic contact sensitization.…”

Section: Introductionmentioning

confidence: 99%

Spinal sensory and motor blockade by intrathecal doxylamine and triprolidine in rats

Tzeng

Chiu

Wang

et al. 2018

Journal of Pharmacy and Pharmacology

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Objectives The aim of this experiment was mainly to examine the effects of intrathecally injected doxylamine and triprolidine, two antihistamine drugs spinal motor and sensory functions. Methods After intrathecally injecting the rats with five different doses, the dose—response curves of spinal sensory and motor block with doxylamine and triprolidine were constructed. In comparison with the local anaesthetic mepivacaine, the quality and duration of spinal anaesthesia with doxylamine or triprolidine were conducted. Key findings Doxylamine, mepivacaine and triprolidine elicited spinal motor and sensory (nociception and proprioception) blockades in a dose‐dependent fashion. On the ED50 (50% effective dose) basis, the rank order of drug potency was triprolidine > mepivacaine > doxylamine (P < 0.05) at provoking spinal motor, proprioceptive and nociceptive blockades. On the equianaesthetic doses (ED25, ED50 and ED75), the duration of spinal anaesthesia with doxylamine was longer (P < 0.01) than that with mepivacaine or triprolidine. Moreover, doxylamine or triprolidine displayed greater potency (ED50) (P < 0.05) and duration (P < 0.05) of sensory block over motor block. Conclusions Doxylamine or triprolidine produces a dose‐dependent effect of spinal motor and sensory block. Triprolidine with a better nociception‐selective action over motor block has a better potency than mepivacaine or doxylamine. Doxylamine and triprolidine produce longer durations than mepivacaine.

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“…Histamine-containing ECL cells are the major endocrine cell type in oxyntic mucosa. Four subtypes of histamine receptors have been identified, termed H1-R, H2-R, H3-R, and H4-R [26]. Histamine, released from ECL cells in response to gastrin, stimulates the parietal cell directly via the H2-R. Histamine induces both a G s -dependent increase in intracellular adenosine 3 0 ,5 0 -cyclic AMP (cAMP) and a G q -dependent increase in intracellular calcium.…”

Section: Histaminementioning

confidence: 99%