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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
Drug that blocks histamine or histamine agonists
activation of the receptor by histamine; by comparison, the inverse agonists bind to the receptor and both block the binding of histamine, and reduce its constitutive
Antihistamine
Antihistaminic drug
the agonist histamine which contains an imidazole ring in its structure. The structural diversity among H3R is limited and all known H3R agonists today
H3_receptor_antagonist
Chemical compound
weak antagonist or inverse agonist at histamine H3 receptors[medical citation needed] and a weak partial agonist at histamine H1 receptors.[medical citation
Betahistine
Compound that activates dopamine receptors
(acetylcholine agonist) Histamine agonist Antonini, Angelo; Poewe, Werner (2007). "Fibrotic heart-valve reactions to dopamine-agonist treatment in Parkinson's
Dopamine_agonist
Chemical compound
Histamine trifluoromethyl toluidide (HTFMT) is a mixed H1/H2 histamine agonist which is significantly more potent than histamine itself. It also produces
Histamine trifluoromethyl toluidide
Histamine_trifluoromethyl_toluidide
Mammalian protein found in Homo sapiens
affecting their activity. The drug betazole is an example of a histamine H2 receptor agonist. Histamine is a ubiquitous messenger molecule released from mast cells
Histamine_H2_receptor
Pharmaceutical compound
BP 2.94, or BP-294, also known as FUB-94, is a histamine H3 receptor agonist which was under development for the treatment of asthma, inflammation, pain
BP_2.94
Pharmaceutical compound
SCH-50971 is a histamine H3 receptor agonist which was under development for the treatment of anxiety disorders, gastrointestinal disorders, and migraine
SCH-50971
Class of drugs
Alpha-adrenergic agonists are a class of sympathetic agents that selectively stimulate alpha adrenergic receptors. The alpha-adrenergic receptor has two
Alpha-adrenergic_agonist
Drugs that block the action of histamine
H1-antihistamines. Virtually all H1-antihistamines function as inverse agonists at the histamine H1-receptor, as opposed to neutral antagonists, as was previously
H1_antagonist
Organic compound involved in immune responses
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
Chemical compound
VUF-8430 is a histamine agonist selective for the H4 subtype. Smith FM, Haskelberg H, Tracey DJ, Moalem-Taylor G (2007). "Role of histamine H3 and H4 receptors
VUF-8430
Pharmaceutical compound
or (1R,2R)-trans-2-(1H-imidazol-4-yl)cyclopropylamine, is a histamine H3 receptor agonist which was under development for the treatment of insomnia and
GT-2203
Histamine receptor
histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is activated by the biogenic amine histamine.
Histamine_H1_receptor
Chemical compound
α-Methylhistamine is a synthetic derivative and a selective histamine H3 receptor agonist. It decreases blood pressure and heart rate in guinea pigs.
Α-Methylhistamine
Mammalian protein found in Homo sapiens
effects on cAMP inhibition and MAPK activity, antagonist on histamine release, and inverse agonist on arachidonic acid release) SCH-50971 H3 receptor antagonists
Histamine_H3_receptor
Chemical compound
Methimepip is a histamine agonist which is highly selective for the H3 subtype. It is the N-methyl derivative of immepip. Kitbunnadaj R, Hashimoto T,
Methimepip
Investigational narcolepsy and hypersomnia drugs
Wakix) – histamine H3 receptor antagonist – idiopathic hypersomnia [4] Sodium oxybate micropump (FT-218; Lumryz; ON-SXB) – GABAB receptor agonist and GHB
List of investigational narcolepsy and hypersomnia drugs
List_of_investigational_narcolepsy_and_hypersomnia_drugs
Pharmaceutical compound
whether it is an agonist or an antagonist. As a metabolite of histamine, it is structurally distinct from other GABAA receptor agonists. Unlike γ-aminobutyric
Imidazoleacetic_acid
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
H2_receptor_antagonist
Chemical compound
Cipralisant (GT-2331, tentative trade name Perceptin) is an extremely potent histamine H3 receptor ligand originally developed by Gliatech. Cipralisant was initially
Cipralisant
Chemical compound
4-Methylhistamine is a histamine agonist selective for the H4 subtype. Lim HD, van Rijn RM, Ling P, Bakker RA, Thurmond RL, Leurs R (September 2005).
4-Methylhistamine
Chemical compound
histamine agonist which is selective for the H1 subtype. Flynn SB, Gristwood RW, Owen DA (January 1979). "Differentiation of the roles of histamine H1-
2-Pyridylethylamine
Chemical compound
and also as a partial agonist at the histamine receptors H1 and H2. UR-AK49 is a pure antagonist at Y4 with no partial agonist effects, and although it
UR-AK49
Compounds found in cannabis
CB2 receptors but acts as an indirect antagonist of cannabinoid agonists. It is an agonist at the 5-HT1A receptor and may promote sleep and suppress arousal
Cannabinoid
Pharmaceutical compound
receptor subtypes [74]. AGX-201 is a histamine receptor modulator that acts as an antagonist at H1 receptors and an agonist at H3 receptors. This dual mechanism
AGX-201
Chemical compound
potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator. Histamine agonists Durant G, Duncan
Impromidine
Medication to treat narcolepsy
daytime sleepiness in adults with narcolepsy. It is an inverse agonist of the histamine H3 receptor. It is the first commercially available medication
Pitolisant
Chemical compound
histamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from full agonist, to antagonist, to inverse agonist in
Proxyfan
Antihistamine medication
loratadine to cause drowsiness, but cetirizine shows superior efficacy in the histamine induced wheal and flare paradigm and tends to produce slightly greater
Cetirizine
Pharmaceutical compound
potential treatment for narcolepsy. It is a member of the histamine H3 receptor antagonist/inverse agonist class of medications. Enerisant functions as a potent
Enerisant
Chemical compound
Amthamine is a histamine agonist selective for the H2 subtype. It has been used in vitro and in vivo to study gastric secretion, as well as other functions
Amthamine
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
Type of receptor ligand or drug that blocks a biological response
inverse agonists because of the discovery of constitutive active receptors; antihistamines for example, originally classified as antagonists of histamine H1
Receptor_antagonist
Chemical compound
Immethridine (developmental code name BP-1-5375) is a histamine agonist selective for the H3 subtype. Cipralisant GT-2203 Kitbunnadaj, R; Zuiderveld,
Immethridine
Substance related to histamine functions
to directly modulate the histamine system in the body or brain. Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines)
Histaminergic
Chemical compound
and histamine H1 receptor. Lisuride is a partial agonist of the D2, D3, D4, 5-HT2A, 5-HT2C, 5-HT5A, and H1 receptors, a full or near-full agonist of the
Lisuride
Class of cell surface receptors
(PAT) ligands, but later work showed this binding corresponded to the histamine H1 receptor; "sigma-3" is not recognized in current nomenclature. The
Sigma_receptor
Agent in biochemistry
efficacy. Receptors for which inverse agonists have been identified include the GABAA, melanocortin, mu opioid, histamine, serotonin, and beta adrenergic receptors
Inverse_agonist
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
Behaviour of substances
physiological agonists to each other. There are several substances that have antihistaminergic action despite not being ligands for the histamine receptor
Physiological agonism and antagonism
Physiological_agonism_and_antagonism
Antihistamine used to treat allergies
a potent H1 antihistamine. It is specifically a potent inverse agonist of the histamine H1 receptor. The drug is also commonly described as possessing
Chlorphenamine
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 narcolepsy
Samelisant
Topics referred to by the same term
Official Unionist Party, a political party in Northern Ireland OUP-16, a histamine agonist drug This disambiguation page lists articles associated with the title
OUP_(disambiguation)
Chemical compound
Immepip is a histamine H3 receptor agonist. Its a synthetic molecule that is not currently used clinically. As of now, it is used in research. Scientist
Immepip
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
Pharmaceutical compound
Adopted Name; developmental code name CEP-26401) is a histamine H3 receptor antagonist and inverse agonist which was under development for the treatment of
Irdabisant
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
Compounds that bind to and activate adrenergic beta-2 receptors
Beta2-adrenergic agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic
Beta2-adrenergic_agonist
Chemical compound
Imetit is a histamine H3 receptor agonist. Garbarg, M; Arrang, JM; Rouleau, A; Ligneau, X; Tuong, MD; Schwartz, JC; Ganellin, CR (1992).
Imetit
Class of drug
Dezocine—agonist/antagonist Pentazocine—agonist/antagonist Phenazocine Buprenorphine—partial agonist Dihydroetorphine Etorphine Butorphanol—agonist/antagonist
Opioid
Antihistamine medication
Levocetirizine is an antihistamine. It acts as an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other
Levocetirizine
Chemical compound
Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist. The histamine H3 receptor is an inhibitory autoreceptor located on histaminergic
Ciproxifan
Antihistamine drug
predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist. This action is responsible for its antihistamine and sedative
Hydroxyzine
Chemical compound
A-349,821 is a potent and selective histamine H3 receptor antagonist (or possibly an inverse agonist). It has nootropic effects in animal studies, although
A-349821
Activator of the muscarinic acetylcholine receptor
A muscarinic acetylcholine receptor agonist, also known as a muscarinic agonist or as a muscarinic agent, is an agent that activates the muscarinic acetylcholine
Muscarinic_agonist
Chemical compound
OUP-16 is a histamine agonist selective for the H4 subtype. Hashimoto, T; Harusawa, S; Araki, L; Zuiderveld, OP; Smit, MJ; Imazu, T; Takashima, S; Yamamoto
OUP-16
Medications that relax muscles of the airways
Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways and resulting in easier breathing
Beta-adrenergic_agonist
First-generation antihistamine used as a short-term sedative and hypnotic (sleep aid)
mouth, among others. As an antihistamine, doxylamine is an inverse agonist of the histamine H1 receptor. As a first-generation antihistamine, it typically
Doxylamine
Antihistamine medication
inverse agonist of the histamine H1 receptor. It is a member of the ethanolamine class of antihistaminergic agents. By reversing the effects of histamine on
Diphenhydramine
Atypical antipsychotic medication
principal pharmacological action is as a functionally selective partial agonist at dopamine D2 receptors, stabilizing dopamine activity by enhancing signaling
Aripiprazole
Medicine preventing a biological response
compete with histamine (Figure 2) to bind to histamine receptors, blocking the allergic response by histamine. They are used in treating histamine-mediated
Drug_antagonism
Chemical compound
NMH may act as a partial agonist or an antagonist for some histamine receptors. NMH may have some modulatory effects on histamine signalling, but it is unlikely
1-Methylhistamine
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
Chemical substance that enables neurotransmission
indirectly. Direct-binding agonists can be further characterized as full agonists, partial agonists, inverse agonists. Direct agonists act similar to a neurotransmitter
Neurotransmitter
Pharmaceutical compound
ALTO-203 is a histamine H3 receptor inverse agonist which is under development for the treatment of major depressive disorder with anhedonia. It was also
ALTO-203
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
Chemical compound
selective histamine antagonist which binds selectively to the H3 subtype. However while VUF-5681 blocks the activity of more potent H3 agonists, recent
VUF-5681
Pharmaceutical compound
serotonin receptor modulator, including as a partial agonist of the serotonin 5-HT2A receptor and as an agonist or antagonist of various other serotonin receptors
JRT_(drug)
Investigational insomnia drugs
LU-2-030; MK-0928; OV-101; THIP) – GABAA receptor agonist GT-2203 – histamine H3 receptor agonist Indiplon (NBI-34060) – GABAA receptor positive allosteric
List of investigational insomnia drugs
List_of_investigational_insomnia_drugs
Drug whose use induces sleep
include histamine H3 receptor agonists like α-methylhistamine, BP 2.94, GT-2203 (VUF-5296), and SCH-50971, adenosine A1 and A2A receptor agonists like adenosine
Hypnotic
Drug that binds to and activates nicotinic acetylcholine receptors
A nicotinic agonist is a drug that mimics the action of acetylcholine (ACh) at nicotinic acetylcholine receptors (nAChRs). The nAChR is named for its
Nicotinic_agonist
Investigational pervasive developmental disorder drugs
AGX-201 (histamine dihydrochloride salt) – histamine H1 receptor antagonist and histamine H3 receptor agonist Aminolevulinic acid/sodium ferrous citrate
List of investigational autism and pervasive developmental disorder drugs
List_of_investigational_autism_and_pervasive_developmental_disorder_drugs
Substance that binds to a receptor to change its response to stimuli
efficacy), or both. Negative types decrease the agonist affinity and/or efficacy. Neutral types don't affect agonist activity but can stop other modulators from
Allosteric_modulator
First generation antihistamine
negligible anticholinergic activity, with 130,000-fold selectivity for the histamine H1 receptor over the muscarinic acetylcholine receptors (for comparison
Mepyramine
Opioid analgesic
doses. Nalbuphine is a mixed agonist/antagonist opioid modulator. Specifically, it acts as a moderate-efficacy partial agonist or antagonist of the μ-opioid
Nalbuphine
Investigational cognition and memory disorder drugs
free radical scavenger [31] Irdabisant (CEP-26401) – histamine H3 receptor antagonist/inverse agonist [32] KTX-0101 (sodium β-hydroxybutyrate) – free radical
List of investigational cognition and memory disorder drugs
List_of_investigational_cognition_and_memory_disorder_drugs
atypical antipsychotic / dopamine receptor partial agonist and serotonin receptor modulator AZD-5213 – histamine H3 receptor antagonist Bifemelane (SON-216) –
List of investigational attention deficit hyperactivity disorder drugs
List_of_investigational_attention_deficit_hyperactivity_disorder_drugs
Drug class
5-HT2C receptor agonists are a class of drugs that activate 5-HT2C receptors. They have been investigated for the treatment of a number of conditions including
5-HT2C_receptor_agonist
Muscle relaxant medication
serotonin and norepinephrine reuptake and to block serotonin, adrenergic, histamine, and muscarinic acetylcholine receptors. Chemically, it is very similar
Cyclobenzaprine
Protein found in humans
5nM, EC50 = 0.9nM, Emax = 98% E-6837 – Full agonist at human 5HT6 receptors E-6801 E-6837 – partial agonist at rat 5-HT6 receptors. Orally active in rats
5-HT6_receptor
Symptom of narcolepsy
by an inverse agonist of the histamine H3 receptor, which enhances histamine release in hypothalamus. An inverse agonist of the histamine H3 is Pitolisant
Cataplexy
Investigational antipsychotics
of action – schizophrenia [69] AGX-201 (histamine dihydrochloride) – non-selective histamine receptor agonist – schizophrenia [70] AMG-579 – phosphodiesterase
List of investigational antipsychotics
List_of_investigational_antipsychotics
Pharmaceutical compound
known as 6-propylterguride or 6-propyl-9,10-dihydrolisuride, is a dopamine agonist of the ergoline family described as a prolactin inhibitor and antiparkinsonian
Proterguride
Chemical compound
as an H1 inverse agonist), meaning that it exerts its pharmacological action by competing with histamine for the H1 subtype histamine receptor. By blocking
Chloropyramine
Antidepressant
antagonism of histamine and serotonin receptors, and inhibition of norepinephrine reuptake. More specifically, it is an antagonist/inverse agonist at most,
Mianserin
Chemical compound
properties, resulting from its agonist activity at the β subtype of the GABAa receptor, antagonist activity at all histamine receptors, inhibition of the
Diproqualone
Chemical compound
GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor
GSK-189254
Serotonin receptor protein distributed in the cerebrum and raphe nucleus
areas such as the hippocampus are postsynaptic receptors. 5-HT1A receptor agonists are involved in neuromodulation. They decrease blood pressure and heart
5-HT1A_receptor
Chemical compound
GPCR target: analysis of preclinical pharmacology of histamine H3 antagonists/inverse agonists". Biochemical Pharmacology. 71 (8): 1103–13. doi:10.1016/j
ABT-239
Protein family
Mivazerol Oxymetazoline (also α1 agonist) Rilmenidine (also I agonist) Romifidine Talipexole (also dopamine agonist) Tasipimidine TDIQ (MDTHIQ, MDA-CR)
Alpha-2_adrenergic_receptor
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
Subtype of serotonin receptor
receptors, and Z3517967757. Quipazine – 5-HT2A agonist but also potent 5-HT3 agonist. SN-22 – partial agonist at all three 5-HT2 subtypes Some benzazepines
5-HT2A_receptor
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
Substance that mimics stimulation of cholinergic receptors
blocker and beta blocker Clonidine (α-receptor agonist, α2 > α1, giving negative feedback) Methyldopa (α2 agonist, giving negative feedback) Propranolol (β-receptor
Parasympathomimetic_drug
Chemical compound
medicine. It behaves as a selective, combined 5-HT2C receptor inverse agonist and α2-adrenergic receptor antagonist (at all three subtypes—α2A, α2B,
S32212
Drug that increases wakefulness
receptor agonists like nicotine Histamine and other histamine H1 receptor agonists also have wakefulness-promoting effects. However, H1 receptor agonists as
Wakefulness-promoting_agent
Investigational chronobiotic drugs
inhibitor LML-134 (LML134) – histamine H3 receptor antagonist Ramelteon (Rozerem; TAK-375) – melatonin MT1 and MT2 receptor agonist Armodafinil (Nuvigil) –
List of investigational chronobiotics
List_of_investigational_chronobiotics
Antihistamine medication
Ketotifen is a selective antihistamine – that is, an inverse agonist of the histamine H1 receptor – and mast cell stabilizer. By preventing the degranulation
Ketotifen
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