2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor
  5. H3 Receptor Isoform

H3 Receptor

 

H3 Receptor Related Products (50):

Cat. No. Product Name Effect Purity
  • HY-B0527A
    Amitriptyline hydrochloride
    		Antagonist 99.94%
    Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
  • HY-12199B
    Pitolisant hydrochloride
    		Antagonist 99.51%
    Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  • HY-14111
    GSK189254A
    		Antagonist 98.59%
    GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
  • HY-B0524
    Betahistine
    		Modulator 99.84%
    Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).
  • HY-B0524A
    Betahistine dihydrochloride
    		Modulator 99.82%
    Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).
  • HY-175367
    H3R antagonist 6
    		Antagonist
    H3R antagonist 6 (Compounds 3) (H3-2406) is a Histamine receptor 3 (H3R) antagonist with an IC50 of 5.6 nM. H3R antagonist 6 labeled with 18F has high radiochemical yield, molar activity and moderate brain uptake, but with an off-target binding to the Sigma-1 receptor. H3R antagonist 6 can be used as a PET radioligand for positron emission tomography imaging for central nervous system (CNS) disorders research.
  • HY-178016
    H3R antagonist 8
    		Antagonist
    H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy.
  • HY-12192
    A-423579
    		Antagonist
    A-423579 is an orally active non-imidazole histamine H3 receptor antagonist. A-423579 exhibits high affinity and good selectivity for human and rat H3 receptors, and possesses both antagonistic and inverse agonistic activities. A-423579 can effectively reduce body weight in obese rodents, with concomitant decreases in fat content, plasma leptin levels, and triglycerides. A-423579 possesses anti-obesity activity and can be used in the research of obesity and related metabolic disorders.
  • HY-101198
    Clobenpropit dihydrobromide
    		Modulator 99.76%
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
  • HY-W014941
    (R)-(-)-α-Methylhistamine dihydrochloride
    		Agonist 99.76%
    (R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.
  • HY-15289
    Ciproxifan maleate
    		Antagonist 99.68%
    Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.
  • HY-106000
    GSK239512
    		Antagonist 99.09%
    GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD).
  • HY-12195
    ABT-239
    		Antagonist 99.23%
    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
  • HY-12190
    JNJ-5207852
    		Antagonist 98.0%
    JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.
  • HY-14880
    Bavisant
    		Antagonist
    Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research.
  • HY-101232
    Tiotidine
    		Antagonist 99.28%
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
  • HY-101173
    Imetit dihydrobromide
    		Agonist 98.16%
    Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with Ki values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC50=25 nM).
  • HY-123532
    JNJ10191584
    		Antagonist 99.95%
    JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
  • HY-12206A
    Thioperamide maleate
    		Antagonist 98.26%
    Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide maleate inhibits [3H]histamine synthesis with a Ki of 31 nM.
  • HY-109968
    Irdabisant
    		Antagonist 99.38%
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment.