Histamine Receptor
Isoform-specific Inhibitors
Histamine Receptor Products
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1291 |
Cetirizine DiHClCetirizine DiHCl (UCB P071) is an antihistamine. |
![]() ![]() Body temperatures of pretreated mice during IgG1-induced PSA in FcγRIIB-/- (n=6 per group) or WT (n=4 per group) mice. |
|
S3208 |
Fexofenadine HClFexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM. |
||
S4253 |
Epinastine HClEpinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis. |
||
S2494 |
Olopatadine HClOlopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine. |
||
S4140 |
Buclizine HClBuclizine HCl (UCB-4445) is an antihistamine and anticholinergic of the piperazine derivative family. |
||
S3052 |
Rupatadine FumarateRupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. |
||
S2024 |
Ketotifen FumarateKetotifen Fumarate is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer. |
||
S3183 |
Amitriptyline HClAmitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
||
S3186 |
Azatadine dimaleateAzatadine (SCH10649) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. |
||
S4131 |
LevodropropizineLevodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex. |
||
S5947 |
AmitriptylineAmitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid. |
||
S4672 |
DimenhydrinateDimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness. |
||
S2308 |
HesperetinHesperetin is a bioflavonoid and, to be more specific, a flavanone. |
||
S4696 |
CarbinoxaMine MaleateCarbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties. |
||
S4240 |
Doxylamine SuccinateDoxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects. |
||
S3176 |
Betahistine 2HClBetahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM. |
||
S1847 |
Clemastine FumarateClemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway. |
![]() ![]() Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), *p < 0.05, **p < 0.01).
|
|
S1245 |
Latrepirdine 2HClLatrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
||
S1358 |
LoratadineLoratadine (SCH29851) is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM. |
||
S3037 |
Bepotastine BesilateBepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
||
S1382 |
Mianserin HClMianserin (ORG GB-94) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression. |
||
S0398New |
AstemizoleAstemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects. |
||
S2552 |
Azelastine HClAzelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis. |
||
S1801 |
Ranitidine HydrochlorideRanitidine (AH19065) is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers. |
||
S1866 |
Diphenhydramine HClDiphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis. |
||
S4012 |
DesloratadineDesloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM. |
||
S1816 |
Chlorpheniramine MaleateChlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM. |
||
S2813 |
Ciproxifan MaleateCiproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. |
||
S1986 |
Meclizine 2HClMeclizine (NSC 28728) is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR. |
||
S2107 |
MizolastineMizolastine (SL 850324) is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. |
||
S1845 |
CimetidineCimetidine (SKF-92334), a histamine congener, competitively inhibits histamine binding to histamine H2 receptors. |
||
S2065 |
LafutidineLafutidine (FRG-8813), a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion. |
||
S1890 |
NizatidineNizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM. |
||
S3146 |
Tripelennamine HClTripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM. |
||
S2044 |
Cyproheptadine HClCyproheptadine HCl is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist. |
||
S4026 |
Hydroxyzine 2HClHydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM. |
![]() ![]() a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM. b, Quantification of sterol levels in OPCs treated with the indicated previously reported enhancers of oligodendrocyte formation (n = 2 wells per condition except DMSO, n = 6). Representative of two independent experiments; for concentrations, see Extended Data Fig. 6g. c, Quantification of EBP enzymatic activity in a biochemical assay. All treatments 10 μM. n = 3 independent enzymatic assays, except DMSO, n = 5. Bars indicate mean; error bars indicate s.d. Sigma H127, p-fluorohexahydro-sila-difenidol.
|
|
S4262 |
EbastineEbastine is a potent H1-histamine receptor antagonist, used for allergic disorders. |
||
S2585 |
Brompheniramine hydrogen maleateBrompheniramine hydrogen maleate is a histamine H1 receptors antagonist. |
||
S2905 |
JNJ-7777120JNJ-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 histamin receptors. |
||
S4008 |
Pemirolast potassiumPemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. |
||
S4849 |
Levocetirizine DihydrochlorideLevocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist. |
||
S5670 |
Chloropyramine hydrochlorideChloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects. |
||
S5659 |
EmedastineEmedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM). |
||
S4139 |
Cyclizine 2HClCyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity. |
||
S5940 |
BepotastineBepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. |
||
S4625 |
AlcaftadineAlcaftadine (Lastacaft, R89674) is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor. |
||
S4045 |
Pheniramine MaleatePheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. |
||
S5479 |
Cloperastine hydrochlorideCloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity. |
||
S5656 |
Diphenylpyraline hydrochlorideDiphenylpyraline hydrochloride is the hydrochloride salt form of diphenylpyraline, which is an antihistamine used in the treatment of allergic rhinitis, hay fever, and allergic skin disorders. |
||
S1880 |
Roxatidine Acetate HClRoxatidine Acetate HCl is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation. |
||
S5718 |
AcrivastineAcrivastine is an antihistamine medicine that relieves the symptoms of allergies. |
||
S5447 |
Triprolidine HydrochlorideTriprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis. |
||
S5647 |
Emedastine DifumarateEmedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. |
||
S5018 |
Mebhydrolin napadisylateMebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies. |
||
S8598 |
S 38093S 38093 is a histamine H3 antagonist/inverse agonist with a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors. |
||
S5926 |
Pitolisant hydrochloridePitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype. |
||
S5649 |
Hydroxyzine pamoateHydroxyzine Pamoate is the pamoate salt form of hydroxyzine, a synthetic piperazine histamine H1-receptor antagonist with anti-allergic, antispasmodic, sedative, anti-emetic and anti-anxiety properties. |
||
S3721 |
BilastineBilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action. |
||
S5662 |
RanitidineRanitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach. |
||
S3120 |
Doxepin HClDoxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. It inhibits CYP2D6 activity in vivo. |
||
S4353 |
TerfenadineTerfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
||
S6435 |
MequitazineMequitazine (LM-209) is a histamine H1 antagonist which competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. |
||
S2078 |
FamotidineFamotidine (MK208) is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions. |
||
S6469 |
ThonzylamineThonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
||
S4293 |
Promethazine HClPromethazine HCl is a potent histamine H1 receptor antagonist, used as a sedative and antiallergic medication. |
||
S1357 |
LidocaineLidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. |
||
S3968 |
HistamineHistamine, an organic nitrogenous compound, is involved in local immune responses regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. It is a potent H1 and H2 receptor agonist. |
||
S4117 |
Histamine PhosphateHistamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors. |
||
S4118 |
Histamine 2HClHistamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2. |
||
S6612 |
Betazole DihydrochlorideBetazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function. |
||
S5498 |
Betahistine mesylateBetahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator. |
||
S6569 |
VUF10460VUF10460 is a histamine H4 receptor agonist. |
||
S5619 |
BetahistineBetahistine is an antivertigo drug that primarily acts as a histamine H1 agonist. |
||
S4382 |
Pyrilamine MaleatePyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1291 |
Cetirizine DiHClCetirizine DiHCl (UCB P071) is an antihistamine. |
![]() ![]() Body temperatures of pretreated mice during IgG1-induced PSA in FcγRIIB-/- (n=6 per group) or WT (n=4 per group) mice. |
|
S3208 |
Fexofenadine HClFexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM. |
||
S4253 |
Epinastine HClEpinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis. |
||
S2494 |
Olopatadine HClOlopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine. |
||
S4140 |
Buclizine HClBuclizine HCl (UCB-4445) is an antihistamine and anticholinergic of the piperazine derivative family. |
||
S3052 |
Rupatadine FumarateRupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively. |
||
S2024 |
Ketotifen FumarateKetotifen Fumarate is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer. |
||
S3183 |
Amitriptyline HClAmitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
||
S3186 |
Azatadine dimaleateAzatadine (SCH10649) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. |
||
S4131 |
LevodropropizineLevodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex. |
||
S5947 |
AmitriptylineAmitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. This product is a waxy solid. |
||
S4672 |
DimenhydrinateDimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness. |
||
S2308 |
HesperetinHesperetin is a bioflavonoid and, to be more specific, a flavanone. |
||
S4696 |
CarbinoxaMine MaleateCarbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties. |
||
S4240 |
Doxylamine SuccinateDoxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects. |
||
S3176 |
Betahistine 2HClBetahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1847 |
Clemastine FumarateClemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway. |
![]() ![]() Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), *p < 0.05, **p < 0.01).
|
|
S1245 |
Latrepirdine 2HClLatrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
||
S1358 |
LoratadineLoratadine (SCH29851) is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM. |
||
S3037 |
Bepotastine BesilateBepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7. |
||
S1382 |
Mianserin HClMianserin (ORG GB-94) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression. |
||
S0398New |
AstemizoleAstemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects. |
||
S2552 |
Azelastine HClAzelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis. |
||
S1801 |
Ranitidine HydrochlorideRanitidine (AH19065) is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers. |
||
S1866 |
Diphenhydramine HClDiphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis. |
||
S4012 |
DesloratadineDesloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM. |
||
S1816 |
Chlorpheniramine MaleateChlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM. |
||
S2813 |
Ciproxifan MaleateCiproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. |
||
S1986 |
Meclizine 2HClMeclizine (NSC 28728) is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR. |
||
S2107 |
MizolastineMizolastine (SL 850324) is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. |
||
S1845 |
CimetidineCimetidine (SKF-92334), a histamine congener, competitively inhibits histamine binding to histamine H2 receptors. |
||
S2065 |
LafutidineLafutidine (FRG-8813), a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion. |
||
S1890 |
NizatidineNizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM. |
||
S3146 |
Tripelennamine HClTripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM. |
||
S2044 |
Cyproheptadine HClCyproheptadine HCl is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist. |
||
S4026 |
Hydroxyzine 2HClHydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM. |
![]() ![]() a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM. b, Quantification of sterol levels in OPCs treated with the indicated previously reported enhancers of oligodendrocyte formation (n = 2 wells per condition except DMSO, n = 6). Representative of two independent experiments; for concentrations, see Extended Data Fig. 6g. c, Quantification of EBP enzymatic activity in a biochemical assay. All treatments 10 μM. n = 3 independent enzymatic assays, except DMSO, n = 5. Bars indicate mean; error bars indicate s.d. Sigma H127, p-fluorohexahydro-sila-difenidol.
|
|
S4262 |
EbastineEbastine is a potent H1-histamine receptor antagonist, used for allergic disorders. |
||
S2585 |
Brompheniramine hydrogen maleateBrompheniramine hydrogen maleate is a histamine H1 receptors antagonist. |
||
S2905 |
JNJ-7777120JNJ-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 histamin receptors. |
||
S4008 |
Pemirolast potassiumPemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. |
||
S4849 |
Levocetirizine DihydrochlorideLevocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist. |
||
S5670 |
Chloropyramine hydrochlorideChloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects. |
||
S5659 |
EmedastineEmedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM). |
||
S4139 |
Cyclizine 2HClCyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity. |
||
S5940 |
BepotastineBepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease. |
||
S4625 |
AlcaftadineAlcaftadine (Lastacaft, R89674) is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor. |
||
S4045 |
Pheniramine MaleatePheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. |
||
S5479 |
Cloperastine hydrochlorideCloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity. |
||
S5656 |
Diphenylpyraline hydrochlorideDiphenylpyraline hydrochloride is the hydrochloride salt form of diphenylpyraline, which is an antihistamine used in the treatment of allergic rhinitis, hay fever, and allergic skin disorders. |
||
S1880 |
Roxatidine Acetate HClRoxatidine Acetate HCl is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation. |
||
S5718 |
AcrivastineAcrivastine is an antihistamine medicine that relieves the symptoms of allergies. |
||
S5447 |
Triprolidine HydrochlorideTriprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis. |
||
S5647 |
Emedastine DifumarateEmedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. |
||
S5018 |
Mebhydrolin napadisylateMebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies. |
||
S8598 |
S 38093S 38093 is a histamine H3 antagonist/inverse agonist with a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors. |
||
S5926 |
Pitolisant hydrochloridePitolisant (Tiprolisant, BF-2649) acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype. |
||
S5649 |
Hydroxyzine pamoateHydroxyzine Pamoate is the pamoate salt form of hydroxyzine, a synthetic piperazine histamine H1-receptor antagonist with anti-allergic, antispasmodic, sedative, anti-emetic and anti-anxiety properties. |
||
S3721 |
BilastineBilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action. |
||
S5662 |
RanitidineRanitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach. |
||
S3120 |
Doxepin HClDoxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. It inhibits CYP2D6 activity in vivo. |
||
S4353 |
TerfenadineTerfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9. |
||
S6435 |
MequitazineMequitazine (LM-209) is a histamine H1 antagonist which competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. |
||
S2078 |
FamotidineFamotidine (MK208) is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions. |
||
S6469 |
ThonzylamineThonzylamine (Neohetramine) is an antihistamine and anticholinergic drug. |
||
S4293 |
Promethazine HClPromethazine HCl is a potent histamine H1 receptor antagonist, used as a sedative and antiallergic medication. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1357 |
LidocaineLidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. |
||
S3968 |
HistamineHistamine, an organic nitrogenous compound, is involved in local immune responses regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. It is a potent H1 and H2 receptor agonist. |
||
S4117 |
Histamine PhosphateHistamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors. |
||
S4118 |
Histamine 2HClHistamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2. |
||
S6612 |
Betazole DihydrochlorideBetazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function. |
||
S5498 |
Betahistine mesylateBetahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator. |
||
S6569 |
VUF10460VUF10460 is a histamine H4 receptor agonist. |
||
S5619 |
BetahistineBetahistine is an antivertigo drug that primarily acts as a histamine H1 agonist. |
||
S4382 |
Pyrilamine MaleatePyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. |