Histamine receptors histamine h1 antagonists. Medical search. Frequent questions

The degree of sleepiness that occurs is generally less than with first-generation antihistamines because second-generation antihistamines are more selective for the H1 receptor. (wikipedia.org)
PET studies with antihistamines have found that brain H1 receptor occupancy of more than 50% is associated with a high prevalence of somnolence and cognitive decline, whereas brain H1 receptor occupancy of less than 20% is considered to be non-sedative. (wikipedia.org)
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)

Cetirizine acts as a highly selective antagonist of the histamine H1 receptor. (wikipedia.org)
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)

Compared to other second-generation anti-histamines, cetirizine can cause drowsiness. (wikipedia.org)
The Ki values for the H1 receptor are approximately 6 nM for cetirizine, 3 nM for levocetirizine, and 100 nM for dextrocetirizine, indicating that the levorotatory enantiomer is the main active form. (wikipedia.org)
Cetirizine has 600-fold or greater selectivity for the H1 receptor over a wide variety of other sites, including muscarinic acetylcholine, serotonin, dopamine, and α-adrenergic receptors, among many others. (wikipedia.org)
A positron emission tomography (PET) study found that brain occupancy of the H1 receptor was 12.6% for 10 mg cetirizine, 25.2% for 20 mg cetirizine, and 67.6% for 30 mg hydroxyzine. (wikipedia.org)
In accordance, H1 receptor occupancy correlated well with subjective sleepiness for 30 mg hydroxyzine but there was no correlation for 10 or 20 mg cetirizine. (wikipedia.org)
As such, brain penetration and brain H1 receptor occupancy by cetirizine are dose-dependent, and in accordance, while cetirizine at doses of 5 to 10 mg have been reported to be non-sedating or mildly sedating, a higher dose of 20 mg has been found to induce significant drowsiness in other studies. (wikipedia.org)
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)

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)

A class of histamine receptors discriminated by their pharmacology and mode of action. (uchicago.edu)

Competes with histamine on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. (medscape.com)

Antiallergic effects of H1-receptor antagonists. (uchicago.edu)

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)
Potent H1 receptor antagonist. (studyhippo.com)
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)

The drug shows 20,000-fold or greater selectivity for the H1 receptor over the five muscarinic acetylcholine receptors, and hence does not exhibit anticholinergic effects. (wikipedia.org)

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)
Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. (drugbank.com)

Lafutidine is a newly developed histamine H(2)-receptor antagonist, which can inhibit gastric acid secretion. (targetmol.com)

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)

Hydroxyzine A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. (scitoys.com)
Bilastine is a peripheral histamine H1-antagonist used to treat seasonal allergic rhinitis and chronic spontaneous urticaria. (drugbank.com)
A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. (nih.gov)

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)

This suppresses the formation of edema and pruritus (caused by histamine). (wikidoc.org)
More basic and clinical studies are needed to address the effects of drugs on specific receptors and improve the treatment of postoperative pruritus. (asahq.org)

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)

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 is an histamine H1-receptor antagonist. (wikidoc.org)
Astemizole competitively binds to histamine H1-receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. (wikidoc.org)
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)
Astemizole may also act on histamine H3 receptors, thereby producing adverse effects. (wikidoc.org)

For instance, Emergo Therapeutics is developing norketotifen, an antagonist of the histamine H1 receptor and mast stabilizer, to treat allergic rhinitis. (technavio.com)
During allergic response mast cells undergo degranulation which releases histamine and other subastances. (drugbank.com)
By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells. (drugbank.com)

Azelastine Hydrochloride exhibits histamine H1-receptor antagonist activity in isolated tissues. (com.bd)

These agents act by competitive inhibition of histamine at the H1 receptor. (medscape.com)

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)

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)

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)
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)
Betahistine hydrochloride is a histamine analog and H1 receptor agonist that serves as a vasodilator. (targetmol.com)

Clemizole hydrochloride is an antagonist for H1 histamine receptor. (targetmol.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)

Because the symptoms of itching and redness in these conditions are caused by histamine acting on the H1 receptor, blocking those receptors temporarily relieves those symptoms. (wikipedia.org)
It is used for symptomatic relief of symptoms caused by release of histamine in allergic reactions. (medscape.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)

It competitively blocks histamine from binding to H1 receptors. (medscape.com)

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)

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)

Among the many responses mediated by these receptors are smooth muscle contraction, increased vascular permeability, hormone release, and cerebral glyconeogenesis. (uchicago.edu)

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)

Regulation of Con A-dependent cytokine production from CD4+ and CD8+ T lymphocytes by autosecretion of histamine. (uchicago.edu)

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)

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)

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)

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)

The CD3 receptor on the surface of T-cells, which helps start an immune response in your body. (oncolink.org)

Receptors, Histamine H1" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uchicago.edu)

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)

The histamine receptors are a class of G protein-coupled receptors which bind histamine as their primary endogenous ligand. (targetmol.com)

This graph shows the total number of publications written about "Receptors, Histamine H1" by people in this website by year, and whether "Receptors, Histamine H1" was a major or minor topic of these publications. (uchicago.edu)
The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity. (com.bd)
Conclusions: The data suggest that the H-1 histamine receptor does not play a major role in the EAR, but is involved in LAR physiological response in the BNR TMA allergic asthma model. (cdc.gov)

In a single-cell RT-PCR study using primers for the two orexin receptors, we found that most tuberomammillary neurons express both receptors and that the expression of the orexin-2 receptor is stronger than that of the orexin-1 receptor. (jneurosci.org)

M 2 receptors are expressed in the heart, hindbrain, smooth muscle and in the synapses of the autonomic nervous system. (justia.com)
M 3 receptors are expressed in the brain, glands and smooth muscle. (justia.com)

Anatomy15

Organisms7

Diseases5

Chemicals and Drugs84

Analytical, Diagnostic and Therapeutic Techniques and Equipment3

Phenomena and Processes14

Information Science2

Antihistamines5

Selective antagonist3

Cetirizine8

Mechanism2

Pharmacology1

Effector cells1

Antiallergic1

Potent3

Muscarinic acetylcho1

Antihistamine4

Gastric Acid Secretion1

Diphenhydramine3

Urticaria3

10mg1

Pruritus2

IC501

Astemizole5

Mast3

Azelastine1

Inhibition1

Blockers1

Inhibitor3

Betahistine3

Hydrochloride1

Serotonin1

Symptoms3

Competitively1

Secretion1

Acetylcholine1

Contraction1

Bronchoconstriction1

Lymphocytes1

Effects1

Modulation1

Nasal2

Treatment3

Cells1

Mesh1

Commonly1

Class1

Major3

Found1

Smooth muscle2