AgonistAntihistaminesCetirizineAstemizoleSuppresses the formation of edemaPharmacologyAntihistamineSelective antagonistEffector cellsProtein-coupled receptorsMechanismAntiallergicMuscarinicDiphenhydramineBetahistineCompetesInhibition10mgPruritusIC50Diamine OxidaseLevocetirizineAllergic rhinitisAzelastineLeukotrieneSymptomsGastricInhibitorHydrochlorideModulationCompetitivelyIntracellularAllergyPotentMeshContractionBronchoconstrictionLymphocytesOrallyCellsNasalTreatmentActiveRelease
Agonist3
- Both animal and clinical studies have shown that co-treatment with betahistine (a histamine H1 receptor agonist/H3 receptor antagonist) is effective in controlling olanzapine-induced weight gain. (edu.au)
- Evidence suggesting that the histamine H3 receptor plays a key role in vestibular compensation comes from studies indicating that betahistine, a histamine-like drug that acts as both a partial histamine H1 receptor agonist and an H3 receptor antagonist, can accelerate the process of vestibular compensation. (uni-frankfurt.de)
- Betahistine hydrochloride is a histamine analog and H1 receptor agonist that serves as a vasodilator. (targetmol.com)
Antihistamines3
- Brompheniramine maleate is a histamine antagonist, specifically an H1-receptor- blocking agent belonging to the alkylamine class of antihistamines. (nih.gov)
- Antihistamines appear to compete with histamine for receptor sites on effector cells. (nih.gov)
- Unlike most classical antihistamines ( HISTAMINE H1 ANTAGONISTS ) it lacks central nervous system depressing effects such as drowsiness. (nih.gov)
Cetirizine2
- Cetirizine is a selective H1 histamine receptor antagonist derived from piperazine. (trdizin.gov.tr)
- Rationale: The effect of Cetirizine, a selective H1-receptor antagonist, was studied in the Brown Norway rat (BNR) model of trimellitic anhydride (TMA) early and late phase allergic asthma. (cdc.gov)
Astemizole6
- Astemizole is a histamine H1-receptor antagonist. (wikipedia.org)
- Astemizole is rapidly absorbed from the gastrointestinal tract and competitively binds to histamine H1 receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. (wikipedia.org)
- Astemizole may also act on histamine H3 receptors, thereby producing adverse effects. (wikipedia.org)
- Terfenadine, an H1-receptor antagonist antihistamine, is similar in structure to astemizole and haloperidol, a butyrophenone antipsychotic. (drugbank.com)
- In contrast, astemizole acts as a histamine H1 receptor (H1R1) antagonist to activate T cells in a non-specific, DC-independent fashion. (bmj.com)
- Astemizole does not cross the blood-brain barrier , and H1 receptor binding is mostly in the peripheral rather than central nervous system (CNS depression is thus minimal). (wikidoc.org)
Suppresses the formation of edema2
- This suppresses the formation of edema and pruritus (caused by histamine). (wikipedia.org)
- This reversible binding of terfenadine to H1-receptors suppresses the formation of edema, flare, and pruritus resulting from histaminic activity. (drugbank.com)
Pharmacology1
- A class of histamine receptors discriminated by their pharmacology and mode of action. (uchicago.edu)
Antihistamine3
- This is a first-generation antihistamine with anticholinergic effects that binds to H1 receptors in the CNS and the body. (medscape.com)
- Dymista (azelastine hydrochloride and fluticasone propionate) is a combination of an antihistamine (H1 receptor antagonist ) and a corticosteroid indicated for the relief of symptoms of seasonal allergic rhinitis in patients 12 years of age and older who require treatment with both azelastine hydrochloride and fluticasone propionate for symptomatic relief. (rxlist.com)
- It is a fixed dose combination product containing an antihistamine (H receptor antagonist ) and a corticosteroid as active ingredients. (rxlist.com)
Selective antagonist2
- Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. (adooq.com)
- Thioperamide maleate is an effective and selective antagonist of H3 receptor (Ki = 4.3 nM) for inhibition of [3H]histamine synthesis (Ki = 31 nM). (targetmol.com)
Effector cells1
- Competes with histamine on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. (medscape.com)
Protein-coupled receptors3
- Histamine and its receptors represent a complex system of immunoregulation with distinct effects mediated by four GPCRs (G protein-coupled receptors HRs 1-4) and their differential expression, which changes according to the stage of cell differentiation and microenvironmental influences. (hindawi.com)
- The pleiotropic effects of histamine are mediated by 4 histamine receptors (HRs), H1R, H2R, H3R, and H4R, which are G protein-coupled receptors. (hindawi.com)
- The histamine receptors are a class of G protein-coupled receptors which bind histamine as their primary endogenous ligand. (targetmol.com)
Mechanism2
- Moreover, histamine H1-receptor antagonists were found to induce apoptosis in tumoral cells but the mechanism is still unclear. (unlp.edu.ar)
- The mechanism of action of levocetirizine is as a Histamine H1 Receptor Antagonist. (targetmol.com)
Antiallergic1
- Antiallergic effects of H1-receptor antagonists. (uchicago.edu)
Muscarinic5
- Cholinergic muscarinic receptors are members of the G-protein coupled receptor super-family and are further divided into 5 subtypes, M 1 to M 5 . (justia.com)
- Muscarinic receptor sub-types are widely and differentially expressed in the body. (justia.com)
- As a consequence of the wide distribution of muscarinic receptors in the body, significant systemic exposure to muscarinic antagonists is associated with effects such as dry mouth, constipation, mydriasis, urinary retention (all predominantly mediated via blockade of M 3 receptors) and tachycardia (mediated by blockade of M 2 receptors). (justia.com)
- A commonly reported side-effect following inhaled administration of therapeutic dose of the current, clinically used non-selective muscarinic antagonists is dry-mouth and while this is reported as only mild in intensity it does limit the dose of inhaled agent given. (justia.com)
- It is controlled by histamine (H1), muscarinic, and serotonin (5-HT3) receptors and is activated by either one of four trigger zones: Vestibular nuclei, Cerebral cortex, Gastrointestinal tract, and Chemoreceptor. (verifiedmarketresearch.com)
Diphenhydramine3
- Diphenhydramine is a H1-histamine receptor antagonist. (chemindustry.com)
- These may include a steroid, a histamine-1 (H1) receptor antagonist (such as diphenhydramine/Benadryl), and an antipyretic (such as acetaminophen/Tylenol). (oncolink.org)
- Diphenhydramine HCl (Benadryl) is a histamine H1 antagonist used as an antitussive and antiemetic. (targetmol.com)
Betahistine1
- This study provided the first evidence that betahistine could act on hepatic H1 receptors via modulation of AMPKα-SREBP-1 and PPARα-dependent pathways to ameliorate olanzapine-induced dyslipidemia in rats. (edu.au)
Competes1
- Terfenadine competes with histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. (drugbank.com)
Inhibition1
- These agents act by competitive inhibition of histamine at the H1 receptor. (medscape.com)
10mg1
- Xonvea is a fixed-dose combination of 10mg doxylamine succinate (histamine H1 receptor antagonist) and 10mg pyridoxine hydrochloride (vitamin B6 pro-drug) formulated as lactose-free, gastro-resistant, delayed-release tablets specifically for the treatment of the condition. (pharmatimes.com)
Pruritus2
- Hydroxyzine A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. (scitoys.com)
- However, in the treatment of diseases such as chronic pruritus, asthma, and allergic rhinitis, the use of selective H4R ligands and/or modulation of H1 and H4 receptor synergism may be more effective for such pathophysiological conditions. (hindawi.com)
IC502
- Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. (adooq.com)
- Ritanserin is a highly effective, relatively selective, long-acting antagonist of 5-HT2 receptor (IC50: 0.9 nM), less active on Histamine H1, Dopamine D2, Adren. (targetmol.com)
Diamine Oxidase1
- degradation of histamine is mediated by the enzyme diamine oxidase (DAO) and histamine N-methyltransferase (HNMT), which catalyses histamine deamination [ 2 , 3 ]. (hindawi.com)
Levocetirizine1
- Levocetirizine is a histamine H1 receptor antagonist. (impileo.com)
Allergic rhinitis3
- For instance, Emergo Therapeutics is developing norketotifen, an antagonist of the histamine H1 receptor and mast stabilizer, to treat allergic rhinitis. (technavio.com)
- HISTAKIND M 10/120MG TABLET reduces the unpleasant symptoms of allergic rhinitis, where fexofenadine acts by antagonizing the effects of histamine (a substance that cause allergic reaction) on the surface of cells and montelukast acts by blocking the leukotriene receptor, thus leading to a relaxation in smooth muscle, which in turn decreases swelling and inflammation in the airways. (netmeds.com)
- A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. (nih.gov)
Azelastine1
Leukotriene3
- HISTAKIND M 10/120MG TABLET is a combination of Fexofenadine and Montelukast which belongs to the group of medicines called Histamine H1 receptor blockers and Leukotriene receptor antagonists respectively. (netmeds.com)
- It is known as a leukotriene receptor antagonist. (impileo.com)
- These include serum tryptase , chromogranin A , plasma prostaglandin D2, histamine, heparin , a variety of random and 24-hour urinary prostaglandins, and urinary leukotriene E4. (medscape.com)
Symptoms3
- It is used for symptomatic relief of symptoms caused by release of histamine in allergic reactions. (medscape.com)
- Histamine, a biogenic vasoactive amine, causes symptoms such as allergies and has a pleiotropic effect that is dependent on its interaction with its four histamine receptors. (hindawi.com)
- This prevents these symptoms associated with histamine release and allergic reactions. (impileo.com)
Gastric1
- Lafutidine is a newly developed histamine H(2)-receptor antagonist, which can inhibit gastric acid secretion. (targetmol.com)
Inhibitor3
- Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor. (adooq.com)
- Osthole, a potential inhibitor of histamine H1 receptor, has been shown to stimulate osteoblast proliferation and differentiation. (targetmol.com)
- Levodropropizine is a histamine receptor inhibitor. (targetmol.com)
Hydrochloride1
- Clemizole hydrochloride is an antagonist for H1 histamine receptor. (targetmol.com)
Modulation1
- Levodropropizine can inhibit histamine receptor, anti-allergic, and reduce a cough by modulation of neuropeptides involved in the cough reflex and by interfering. (targetmol.com)
Competitively1
- It competitively blocks histamine from binding to H1 receptors. (medscape.com)
Intracellular2
- Results: Expression levels for histamine H3 receptor (total) as well as three isoforms which display variable lengths of the third intracellular loop of the receptor were analyzed using in situ hybridization on brain sections containing the rat medial vestibular nucleus after unilateral labyrinthectomy. (uni-frankfurt.de)
- In this review, we discuss the dualistic effects of histamine: how histamine affects inflammation of the immune system through the activation of intracellular pathways that induce the production of inflammatory mediators and cytokines in different immune cells and how histamine exerts regulatory functions in innate and adaptive immune responses. (hindawi.com)
Allergy2
- Inflammatory conditions (e.g., allergy, asthma, and autoimmune diseases) have long been thought to be mainly mediated by the activation of histamine receptor 1 (H1R). (hindawi.com)
- Histamine shows a dichotomous nature, whereby it is able to promote inflammatory and regulatory responses that contribute to pathological processes, such as allergy induction, as well as homeostatic functions, such as intestinal regulation. (hindawi.com)
Potent1
- JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other hi. (targetmol.com)
Mesh1
- Receptors, Histamine H1" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uchicago.edu)
Contraction2
- In the airways, stimulation of M 3 receptors evokes contraction of airway smooth muscle leading to bronchoconstriction, while in the salivary gland M 3 receptor stimulation increases fluid and mucus secretion leading to increased salivation. (justia.com)
- Among the many responses mediated by these receptors are smooth muscle contraction, increased vascular permeability, hormone release, and cerebral glyconeogenesis. (uchicago.edu)
Bronchoconstriction1
- Both histamine and PAF cause bronchoconstriction which leads to an increase in the vascular permeability and act as a mediator in the inflammatory process. (aristopharma.com)
Lymphocytes1
- Regulation of Con A-dependent cytokine production from CD4+ and CD8+ T lymphocytes by autosecretion of histamine. (uchicago.edu)
Orally1
- Avacopan (CCX168) is an orally administered and selective C5a receptor (C5aR) antagonist. (adooq.com)
Cells1
- The CD3 receptor on the surface of T-cells, which helps start an immune response in your body. (oncolink.org)
Nasal2
- The nasal decongestant effect is mediated by the action of pseudoephedrine on α-sympathetic receptors, producing vasoconstriction of the dilated nasal arterioles. (nih.gov)
- Comparison of the secretory response of the nasal mucosa to methacholine and histamine. (uchicago.edu)
Treatment4
- The newer GABA-effective hypnotics are the only medications with demonstrated effectiveness in treating chronic insomnia with the majority of evidence supporting treatment efficacy for cognitive-behavioral therapy and short acting GABA-receptor agonists. (springer.com)
- Hepatic AMP-activated protein kinase α (AMPKα) was activated in the O + B co-treatment group, with a significant reduction in nuclear SREBP-1 protein expression but an increased expression of peroxisome proliferator-activated receptor-α (PPARα) and its-responsive molecule(CPT1A), compared with olanzapine-only treatment. (edu.au)
- In addition, olanzapine significantly increased hepatic histamine H1 receptors, while O + B co-treatment significantly reversed them to normal levels. (edu.au)
- These antagonists are utilized for the treatment of nausea and vomiting, unusually caused by radiation therapy, chemotherapy, or postoperatively. (verifiedmarketresearch.com)
Active1
- The active and inactive conformations of these receptors coexist in equilibrium. (hindawi.com)
Release1
- M 2 receptors expressed on smooth muscle are understood to be pro-contractile while pre-synaptic M 2 receptors modulate acetylcholine release from parasympathetic nerves. (justia.com)