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Conessine, a steroidal alkaloid, is a potent and selective histamineH3receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H3receptor, respectively. Anti-malarial activity .
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM .
GT-2016 is a potent, selective, and brain penetrant histamineH3receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase .
JNJ-10181457 is a selective non-imidazole histamineH3receptor antagonist that normalizes acetylcholine neurotransmission . JNJ-10181457 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
VUF 5681 dihydrobromide is a neutral antagonist of histamineH3receptor. VUF 5681 dihydrobromide also has partial agonist function of H3receptor. VUF 5681 dihydrobromide blocks the effects of Thioperamide (HY-12206). VUF 5681 dihydrobromide is used in central nervous system disease research .
Immethridine dihydrobromide is a selective histamineH3receptor(H3R) agonist. Immethridine dihydrobromide displays 300-fold selectivity over the H4 receptor and does not bind to H1 or H2 receptors. Immethridine dihydrobromide can be used for experimental autoimmune encephalomyelitis (EAE) research .
A 331440 hydrochloride is a histamineH3receptor antagonist. A 331440 hydrochloride binds potently and selectively to human and rat histamineH3receptors (Ki≤25 nM). A 331440 hydrochloride can be used for antiobesity research .
Enerisant is a potent, highly selective, competitive and orally active histamineH3receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamineH3receptors, respectively .
Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamineH3receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamineH3receptors, respectively .
GSK189254A (GSK189254) is a novel, potent and selective histamineH3receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, high affinity histamineH3receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamineH3receptor and a Ki of 0.47 nM for rat histamineH3receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamineH3receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamineH3receptor and a Ki of 0.47 nM for rat histamineH3receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PF-03654764 is an orally active, selective histamineH3receptor antagonist with Ki values of 1.2 nM and 7.9 nM for human H3 and rat H3 in whole cell assay, respectively. The combination of PF-03654764 and Fexofenadine (HY-B0801A) has the potential for allergic rhinitis research .
KSK94 is a high-affinity histamineH3receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .
Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3receptor antagonist . Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA) .
Betahistine is an orally active histamine H1 receptor agonist and a H3receptor antagonist . Betahistine is used for the study of rheumatoid arthritis (RA) .
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3receptor antagonist . Betahistine mesylate is used for the study of rheumatoid arthritis (RA) .
KSK68 is a high-affinity dual sigma-1 and histamineH3receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histaminereceptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .
Clobenpropit is a potent histamineH3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock .
KSK67 is a high-affinity dual sigma-2 and histamineH3receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .
Iodophenpropit dihydrobromide is a potent and selective histamineH3receptor antagonist. The binding of [ 125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM) .
Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3receptor, respectively, and a pKd of 9.4 for H1 receptor.
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3receptor 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 .
Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamineH3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease .
Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamineH3-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 .
Betahistine-d3 (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine . Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3receptor antagonist used for the study of rheumatoid arthritis (RA) .
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamineH3receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .
Bavisant (JNJ-31001074) dihydrochloride is an orally active, potent, brain-penetrating and highly selective antagonist of the histamineH3receptor. Bavisant dihydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research .
Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamineH3receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .
ABT-288 is a competitive, potent and selective histamineH3receptor(H3R) antagonist. ABT-288 has Ki values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research. .
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamineH3 and H4receptors, 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) .
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3histaminereceptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats .
Tiotidine (ICI 125211) is a potent and selective antagonist of histamineH2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3receptors .
Betahistine- 13C,d3 (dihydrochloride) is the 13C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3histaminereceptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats .
Anticancer agent 192 (compound XXI) is a steroid-based histamineH3receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
JNJ10191584 (VUF6002) is an orally active and selective histamineH4receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4receptor over H3receptor 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 .
PF-03654746 Tosylate is a potent and selective histamineH3receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms . PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
H3R antagonist 2 (Compound 23) is a multitarget histamineH3receptor(H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB .
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamineH4receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4receptor over the H3receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively .
PF-03654746 is a potent and selective histamineH3receptor antagonist with high brain penetration.
PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis .
PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
Samelisant (SUVN-G3031) is a potent and selective histamineH3receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamineH3receptor antagonist (rat Ki=0.47 nM) . Cipralisant (enantiomer) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Samelisant (SUVN-G3031) free base is a potent and selective histamineH3receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamineH3receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamineH3receptor (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 .
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamineH3receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
Clobenpropit dihydrobromide is a potent histamineH3R antagonist/inverse agonist with a pEC50 of 8.07 for histamineH3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4receptors (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 .
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histaminereceptors, H1R, H2R, and H3R .
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor(H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease .
Conessine, a steroidal alkaloid, is a potent and selective histamineH3receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H3receptor, respectively. Anti-malarial activity .
HRH3-VLPs protein, part of the H3 subclass of histamine receptors, potentially mediates histamine signals in the CNS and peripheral nervous system. It inhibits adenylate cyclase, showing constitutive activity even without agonists. Notably, isoform 3 stimulation does not affect adenylate cyclase activity or induce intracellular calcium mobilization. HRH3-VLPs Protein, Human (HEK293, His) is the recombinant human-derived HRH3-VLPs protein, expressed by HEK293 , with C-10*His labeled tag. The total length of HRH3-VLPs Protein, Human (HEK293, His) is 445 a.a., with molecular weight of 50.0 kDa.
HRH3-VLPs protein, part of the H3 subclass of histamine receptors, potentially mediates histamine signals in the CNS and peripheral nervous system. It inhibits adenylate cyclase, showing constitutive activity even without agonists. Notably, isoform 3 stimulation does not affect adenylate cyclase activity or induce intracellular calcium mobilization. HRH3-VLPs Protein, Human (HEK293, GFP) is the recombinant human-derived HRH3-VLPs protein, expressed by HEK293 , with C-GFP labeled tag. The total length of HRH3-VLPs Protein, Human (HEK293, GFP) is 445 a.a., with molecular weight of 75.9 kDa.
Betahistine-d3 (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
Betahistine- 13C,d3 (dihydrochloride) is the 13C- and deuterium labeled Betahistine (dihydrochloride). Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3receptor antagonist[1]. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA)[3].
