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Class of receptor proteins that bind histamine
The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand. Histamine is a neurotransmitter
Histamine_receptor
Histamine receptor
The H1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is activated by the biogenic
Histamine_H1_receptor
Drug that blocks histamine or histamine agonists
activity of histamine receptors in the body. In this sense of the word, antihistamines are subclassified according to the histamine receptor that they act
Antihistamine
Mammalian protein found in Homo sapiens
Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act as autoreceptors
Histamine_H3_receptor
Class of medications
blockers, are a class of medications that block the action of histamine at the histamine H2 receptors of the parietal cells in the stomach. This decreases the
H2_receptor_antagonist
Mammalian protein found in Homo sapiens
H2 receptors are a type of histamine receptor found in many parts of the anatomy of humans and other animals. They are positively coupled to adenylate
Histamine_H2_receptor
Mammalian protein found in Homo sapiens
The histamine H4 receptor, like the other three histamine receptors, is a member of the G protein-coupled receptor superfamily that in humans is encoded
Histamine_H4_receptor
Monoamine neurotransmitter
Histamine or histamin is an organic nitrogenous compound found in mammals and many vegetables, fruits and food products. It consists of an imidazole ring
Histamine
Drugs that block the action of histamine
blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main
H1_antagonist
Antihistaminic drug
An H3 receptor antagonist is a type of antihistaminic drug used to block the action of histamine at H3 receptors. Unlike the H1 and H2 receptors which
H3_receptor_antagonist
Compound that activates dopamine receptors
A dopamine agonist is a compound that activates dopamine D2 receptors and belong to one of two different subclasses: ergoline and non-ergoline. Examples
Dopamine_agonist
Type of receptor ligand or drug that blocks a biological response
but act at different receptors. For example, histamine lowers arterial pressure through vasodilation at the histamine H1 receptor, while adrenaline raises
Receptor_antagonist
Antihistamine medication
breastfeeding is not recommended. The medication works by blocking histamine H1 receptors, mostly outside the brain. Cetirizine can be used for paediatric
Cetirizine
Group of pharmaceuticals that modulate the renin–angiotensin system
Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin
Angiotensin II receptor blocker
Angiotensin_II_receptor_blocker
Compounds found in cannabis
suggests additional receptors may exist. The human brain has more cannabinoid receptors than any other G protein-coupled receptor (GPCR) type. The endocannabinoid
Cannabinoid
Class of pharmacological agents
class of pharmacological agents that act as antagonists on α-adrenergic receptors (α-adrenoceptors). Historically, alpha-blockers were used as a tool for
Alpha_blocker
Drug which blocks dopamine receptors
anti-dopaminergic and a dopamine receptor antagonist (DRA), is a type of drug which blocks dopamine receptors by receptor antagonism. Most antipsychotics
Dopamine_antagonist
Class of anesthetics
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the N-methyl-D-aspartate receptor (NMDAR). They are commonly
NMDA_receptor_antagonist
Substance related to histamine functions
directly modulate the histamine system in the body or brain. Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines)
Histaminergic
Drug to increase activity at histamine receptors
A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes. H1 agonists promote wakefulness
Histamine_agonist
Science of drugs and medications and their effects
broad terms, pharmacodynamics discusses the chemicals with biological receptors, and pharmacokinetics discusses the liberation, absorption, distribution
Pharmacology
Drug that binds to and activates nicotinic acetylcholine receptors
that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its affinity for nicotine. Examples include
Nicotinic_agonist
Class of drugs
selectively stimulate alpha adrenergic receptors. The alpha-adrenergic receptor has two subclasses, α1 and α2. Alpha 2 receptors are associated with sympatholytic
Alpha-adrenergic_agonist
Pharmaceutical compound
AGX-201, also known as histamine dihydrochloride, is a histamine receptor modulator which is under development for the treatment of migraine. It is or
AGX-201
Drug that binds to but does not activate muscarinic cholinergic receptors
Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL (2003). "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical
Muscarinic_antagonist
Parasympathetic nervous system inhibitors
parasympathetic nervous system by selectively blocking the binding of ACh to its receptor in nerve cells. The nerve fibers of the parasympathetic system are responsible
Anticholinergic
Category of drug
A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other
GABA_receptor_agonist
Regulation of neurons by neurotransmitters
the central nervous system include: dopamine, serotonin, acetylcholine, histamine, norepinephrine, nitric oxide, and several neuropeptides. Cannabinoids
Neuromodulation
Drug that stimulates a response from the adrenergic receptors
that stimulates a response from the adrenergic receptors. The five main categories of adrenergic receptors are: α1, α2, β1, β2, and β3, although there are
Adrenergic_agonist
Substance that binds to a receptor to change its response to stimuli
allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimuli. Some of them, like benzodiazepines or
Allosteric_modulator
Chemical compound
and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki = 0.2nM) and selectivity
GSK-189254
Chemical agents that inhibit Cholinesterase
neuromuscular junctions, the synaptic clefts of which are rich in acetylcholine receptors. ChEIs are indirect-acting parasympathomimetic drugs. Both the acetylcholinesterase
Cholinesterase_inhibitor
Substance that mimics stimulation of cholinergic receptors
parasympathomimetic drug, sometimes called a cholinomimetic drug or cholinergic receptor stimulating agent, is a substance that stimulates the parasympathetic nervous
Parasympathomimetic_drug
Chemical compound class
antagonists to prevent nausea and vomiting. The discovery of neurokinin 1 (NK1) receptor antagonists was a turning point in the prevention of nausea and vomiting
NK1_receptor_antagonist
Activator of the muscarinic acetylcholine receptor
acetylcholine receptor agonist, also known as a muscarinic agonist or as a muscarinic agent, is an agent that activates the muscarinic acetylcholine receptor. The
Muscarinic_agonist
Medications that relax muscles of the airways
muscle relaxation and contraction of the cardiac tissue. Activation of β1 receptors induces positive inotropic, chronotropic output of the cardiac muscle
Beta-adrenergic_agonist
Type of ion channel transmembrane protein
Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow
Ligand-gated_ion_channel
Pharmaceutical compound
United States Adopted Name; developmental code name CEP-26401) is a histamine H3 receptor antagonist and inverse agonist which was under development for the
Irdabisant
Class of enzymes
Histamine N-methyltransferase (HNMT) is a protein encoded by the HNMT gene in humans. It belongs to the methyltransferases superfamily of enzymes and
Histamine_N-methyltransferase
Compounds that bind to and activate adrenergic beta-2 receptors
agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic agonists, they
Beta2-adrenergic_agonist
Medication
Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid production. It is mainly used
Cimetidine
Type of paralyzing anesthetic including lepto- and pachycurares
accomplished via their action on the post-synaptic acetylcholine (Nm) receptors. In clinical use, neuromuscular block is used adjunctively to anesthesia
Neuromuscular-blocking_drug
Presumed set of adverse reactions
Histamine intolerance is a presumed set of adverse reactions (such as flushing, itching, rhinitis, etc.) to ingested histamine in food. The mainstream
Histamine_intolerance
Substance related to dopamine functions
dopamine receptors can be classified as dopaminergic, and neurons that synthesize or contain dopamine and synapses with dopamine receptors in them may
Dopaminergic
Substance having effect(s) on the body of an individual
glutamate receptor modulators Monoamines: Adrenergic receptor modulators Dopamine receptor modulators Histamine receptor modulators Melatonin receptor modulators
Drug
Drug that inhibits the action of acetylcholine at nicotinic acetylcholine receptors
inhibits the action of acetylcholine (ACh) at nicotinic acetylcholine receptors. These compounds are mainly used for peripheral muscle paralysis in surgery
Nicotinic_antagonist
Anti-nausea group of medications
and have little affinity for other receptors, such as dopamine, histamine and muscarinic acetylcholine receptors. All 5-HT3 antagonists are well-absorbed
5-HT3_antagonist
Neurotransmission-modulating substance
needed] Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and a1 adrenoreceptors. Ketanserin Antihypertensive. Blocks 5-HT2A
Serotonin_receptor_antagonist
Gastrointestinal system drug
Betazole (also known as ametazole) is a histamine H2 receptor agonist. Betazole hydrochloride is known as gastramine and histalog. It has been used as
Betazole
Antihistamine used to treat allergies
It is a first-generation antihistamine and works by blocking the histamine H1 receptor. Common side effects include sleepiness, restlessness, and weakness
Chlorphenamine
Antihistamine drug
Hydroxyzine's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action is responsible for its antihistamine
Hydroxyzine
Class of compounds
Alpha-1-adrenergic receptors are present in vascular smooth muscle, the central nervous system, and other tissues. When alpha blockers bind to these receptors in vascular
Alpha-1_blocker
Agent which mimics choline
behaviours at one or more of the body's acetylcholine receptor ("direct-acting") or butyrylcholine receptor types ("direct-acting"). Such mimics are called
Cholinergic
Immune cell found in connective tissue
contains many small secretory granules for the storage and release of histamine, heparin and other mediators. Derived from myeloid progenitor cells, mast
Mast_cell
Medication to treat narcolepsy
sleepiness in adults with narcolepsy. It is an inverse agonist of the histamine H3 receptor. It is the first commercially available medication in its class;
Pitolisant
Type of drug
receptors. There are five adrenergic receptors, which are divided into two groups. The first group of receptors are the beta (β) adrenergic receptors
Adrenergic_antagonist
Behaviour of substances
histamine, which lowers arterial pressure. Thus, despite not being true antihistamines because they do not bind to and block the histamine receptor,
Physiological agonism and antagonism
Physiological_agonism_and_antagonism
Neurotransmission-modulating substance
A serotonin receptor agonist is an agonist of one or more serotonin receptors. They activate serotonin receptors in a manner similar to that of serotonin
Serotonin_receptor_agonist
Medication that reduces stomach acid
Famotidine, sold under the brand name Pepcid among others, is a histamine H2 receptor antagonist medication that decreases stomach acid production. It
Famotidine
Affecting GABA systems in the brain
Dopamine receptor agonist Dopamine receptor antagonist Dopamine reuptake inhibitor (DRI) Histaminergic Histamine receptor agonist Histamine receptor antagonist
GABAergic
Type of drug
and they exert these effects by binding to and activating the transient receptor potential cation channel TRPC6. Activation of TRPC6 induces the entry of
Reuptake_inhibitor
Pertaining to adrenaline or noradrenaline, or their receptors
adrenaline (epinephrine) or noradrenaline (norepinephrine)" (or on their receptors). When not further qualified, it is usually used in the sense of enhancing
Adrenergic
Atypical antipsychotic medication
and 5-HT1F receptor ligand α1- and α2-adrenergic receptor antagonist Histamine H1 receptor antagonist Muscarinic acetylcholine receptor antagonist This
Quetiapine
Drugs blocking alpha-2 adrenergic receptors
alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly used in research, having found limited clinical application
Alpha-2_blocker
Measure of relative response to a drug
(IA) and maximal efficacy (Emax) refer to the relative ability of a drug-receptor complex to produce a maximum functional response. This must be distinguished
Intrinsic_activity
Chemical compound
antihistamine used to help prevent itching of the eyes. It is an H1 histamine receptor antagonist. It is given as an drops in the eye. It was approved for
Alcaftadine
Antihistamine medication
second-generation antihistamine and takes effect by selectively inhibiting the histamine H1 receptor, preventing these allergic reactions. Bilastine has an effectiveness
Bilastine
Type of medication
adrenergic receptors. However, there are exceptions: guanfacine and clonidine are adrenergic agonists at the α2 receptor; since this receptor is located
Sympatholytic
Pharmaceutical compound
Name; developmental code names BEN-2001 and JNJ-31001074) is a histamine H3 receptor receptor antagonist which was under development for the treatment of
Bavisant
Class of drugs
An adenosine receptor agonist is a drug which acts as an agonist of one or more of the adenosine receptors. Examples include the neurotransmitter adenosine
Adenosine_receptor_agonist
Type of organic compounds
protein–coupled receptor-X2 (MRGPRX2) in cutaneous mast cell is the only proven mechanism of direct mast cell degranulation that corresponds to proposed histamine liberators
Histamine_liberators
Chemical compound
by competing with histamine for the H1 subtype histamine receptor. By blocking the effects of histamine, the drug inhibits the vasodilation, increased
Chloropyramine
Antihistamine medication
agonist of the histamine H1 receptor. It is a member of the ethanolamine class of antihistaminergic agents. By reversing the effects of histamine on the capillaries
Diphenhydramine
Chemical compound
Dimaprit is a histamine analog working as a selective H2 histamine receptor agonist. Kartzung, Betram G.; Trevor, Anthony J., eds. (2014). Basic and Clinical
Dimaprit
Epithelial cell in the stomach
of histamine through H2 receptor causes increases in the intracellular cAMP level, while ACh through M3 receptor and gastrin through CCK2 receptor increases
Parietal_cell
Chemical compound
novel histamine receptor ligands. Binding assays determined that (-)-trans-H2-PAT possessed the strongest binding affinity at the histamine H1 receptor. Booth
Phenylaminotetralin
First generation antihistamine
the histamine H1 receptor over the muscarinic acetylcholine receptors (for comparison, diphenhydramine had 20-fold selectivity for the H1 receptor). Mepyramine
Mepyramine
Molecule able to block protein channels, frequently used as pharmaceutical
to their pore also exist: 5-HT3 receptor antagonists GABAA receptor antagonists nACh receptor antagonists NMDA receptor antagonists Channel blockers are
Channel_blocker
Enzyme
"Biological and Pharmacological Aspects of Histamine Receptors and Their Ligands". Biomedical Aspects of Histamine. Springer. pp. 61–100. doi:10.1007/978-90-481-9349-3_4
Diamine_oxidase
Substance that binds to and regulates the activity of chemical receptors
A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical
Receptor_modulator
Chemical compound
is a Histamine H1 receptor antagonist: selectively binding to but not activating the receptor, thereby blocking the actions of endogenous histamine and
Antazoline
Drug used to prevent nausea or vomiting
another recently approved drug from this class Antihistamines (H1 histamine receptor antagonists) are effective in many conditions, including motion sickness
Antiemetic
Class of cell surface receptors coupled to G-protein-associated intracellular signaling
protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G
G_protein-coupled_receptor
Tricyclic antidepressant
Weizel L, Ligneau X, Stark H (January 2009). "Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics". Bioorganic & Medicinal
Amitriptyline
Chemical compound
has antisecretory and bactericidal action. Group affiliation: H2-histamine receptor blocker. Pills. The film-coated tablet contains ranitidine bismuth
Ranitidine_bismuth_citrate
Agent that interferes with action at the vasopressin receptors
A vasopressin receptor antagonist (VRA) is an agent that interferes with action at the vasopressin receptors. Most commonly VRAs are used in the treatment
Vasopressin receptor antagonist
Vasopressin_receptor_antagonist
Chemical compound
code SKF 92994) is an H2 histamine receptor receptor antagonist. Willson RA, Hall T, Hart J (June 1988). "Oxmetidine (H2 receptor antagonist) induced cytotoxicity
Oxmetidine
First-generation antihistamine used as a short-term sedative and hypnotic (sleep aid)
others. As an antihistamine, doxylamine is an inverse agonist of the histamine H1 receptor. As a first-generation antihistamine, it typically crosses the blood–brain
Doxylamine
Class of cell surface receptors
ligands, but later work showed this binding corresponded to the histamine H1 receptor; "sigma-3" is not recognized in current nomenclature. The fungal
Sigma_receptor
Atypical antipsychotic medication
BA, Renock SM, Steinberg S, Ernsberger P, et al. (March 2003). "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical
Aripiprazole
Antihistamine medication
This blocking prevents the binding of histamine to these receptors and thus reduces the symptoms of histamine-mediated reactions, such as itching, sneezing
Ketotifen
Compounds that inhibit or block the activity of cannabinoid receptors
A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of cannabinoidergic drug that binds
Cannabinoid receptor antagonist
Cannabinoid_receptor_antagonist
Chemical substance that enables neurotransmission
Voltage- gated Ca++ channel Synaptic vesicle Neurotransmitter transporter Receptor Neurotransmitter Axon terminal Synaptic cleft Dendrite A neurotransmitter
Neurotransmitter
Chemical compound
PMC 12406145. PMID 40892398. Ricke DO (4 February 2026). "Mast cells and histamine receptor-targeted adjunctive treatments for COVID-19: A literature review"
Azelastine
Antidepressant medication
agonist and antagonist of various serotonin receptors, antagonist of adrenergic receptors, weak histamine H1 receptor antagonist, and weak serotonin reuptake
Trazodone
Antidepressant medication
affinity of the drug for the histamine H1, 5-HT2A, and 5-HT2C receptors; exhibiting near exclusive occupation of these receptors at doses ≤15 mg. However
Mirtazapine
Chemical substance that alters brain function
Sakamoto Y, Sakurai T, Yamatodani A (2003-03-20). "Modafinil increases histamine release in the anterior hypothalamus of rats". Neuroscience Letters. 339
Psychoactive_drug
Experimental drug to treat narcolepsy
experimental wakefulness-promoting agent acting as a selective histamine H3 receptor inverse agonist which is under development for the treatment of
Samelisant
Adrenergic receptors – bound by epinephrine (adrenaline) and norepinephrine (noradrenaline) Dopamine receptors – bound by dopamine Histamine receptors – bound
Monoamine_receptor
Medication that decreases stomach acid
Clostridioides difficile colitis. Ranitidine is an H2 histamine receptor antagonist that works by blocking histamine, thus decreasing the amount of acid released
Ranitidine
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HISTAMINE RECEPTOR
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