histamine receptor 3

H3 receptor-MO-1, a potent modulator of the histamine H3 receptor (H3 receptor), can be utilized to study neurodegeneration and cognitive disorders.

PF 03654746 FA is a human histamine receptor H(3) antagonist that can be used to study cognitive impairment and Alzheimer's disease.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea

Epinastine (WAL801), a potent, selective, and orally-active antihistamine and mast cell stabilizer, functions as a histamine H1 receptor antagonist. It also inhibits IL-8 release from human eosinophils, showcasing antiallergic action [1] [2] [3] [4].

VUF10460, a non-imidazole histamine H4 receptor agonist, [58C8-51-20-3] is structurally classified under the chlorobenzylpiperazine ethers with the IUPAC designation (2-[(2-chlorophenyl)methyl]-1-piperazinyl)(1H-indol-3-yl)methanone. It is typically utilized in pharmacological research and exhibits specificity for the H4 subtype, making it a valuable tool in immunological studies.

LML134 (LML-134) is an inverse agonist of Histamine 3 receptor (H3R)(hH3R cAMP and hH3R bdg with Kis of 0.3 nM and 12 nM).

Chloropyramine hydrochloride (Alergosan) is a histamine receptor H1 antagonist.

Doxepin D3 Hydrochloride is a deuterium-labeled doxepin hydrochloride.Doxepin hydrochloride is an oral active tricyclic antidepressant used as a sedative.Doxepin hydrochloride is also an effective CYP450 inhibitor, significantly inhibiting CYP450 2C19 and

H3R-IN-1 Hydrochloride is an inverse agonist of histamine receptor 3( H3R ) .

H3R-IN-1 is an effective inverse agonist of the histamine receptor 3 (H3R).

HDAC6-IN-49 (Compound 3) is an inhibitor of HDAC, with IC50 values of 0.012 and 0.735 µM against HDAC6 and HDAC1, respectively. Additionally, it inhibits MAO-B, cholinesterase (ChE), histamine receptor (H3R), and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective effects in SH-SY5Y cells and enhances cognitive functions and motor abilities in fruit fly models of Parkinson's disease and C. elegans models of Alzheimer's disease.

GSK-1004723 is a novel antagonist of histamine H(1) and H(3) receptor. It represents a potential novel therapy for allergic rhinitis.

JNJ-28583867 is an inhibitor of histamine H(3) receptor antagonist and serotonin reuptake.

VUF 8328 is an agonist of histamine H(3) receptor.

A-304121 is a histamine H(3) receptor.

3-hydroxy Desloratidine is a major metabolite of desloratadine , a tricyclic antagonist of the histamine H1 receptor.

Tripelennamine, an ethylenediamine derivative, acts as a potent histamine H1-receptor antagonist, effectively reducing the organism's allergic response to histamine. It is utilized in researching conditions such as rhinitis, conjunctivitis, and allergic and anaphylactic reactions [1] [2] [3].

Brompheniramine ((±)-Brompheniramine) is a potent, orally active alkylamine class antihistamine and a selective antagonist of the histamine H1 receptor (Kd = 6.06 nM). It has applications in the research of allergic rhinitis and exhibits anticholinergic, antidepressant, and anesthetic properties. Brompheniramine blocks calcium channels, sodium channels, and hERG channels with IC50 values of 16.12 μM, 21.26 μM, and 0.90 μM, respectively [1] [2] [3] [4].

Izuforant (JW1601) (Compound 24) exhibits potent anti-inflammatory and anti-pruritic activities, with a binding affinity for human serotonin 3 receptor (h5-HT3R) and an IC50 value of 9.1 μM. It is also an orally active antagonist of histamine H4 receptor (H4R), showing an IC50 value of 36 nM against human H4R [1] [2].

Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.

Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in rat brain and peripheral tissues. It reduces isolation-induced aggressive behavior and inhibits electrical foot-shock stimulation-induced belligerence in mice when administered at doses ranging from 3 to 10 mg kg. Maprotiline also reduces aggressive behavior in rhesus monkeys housed in groups. Formulations containing maprotiline have been used in the treatment of depression and anxiety.

Desmethylazelastine, the primary active metabolite of Azelastine, undergoes oxidative metabolism via the cytochrome P450 enzyme system, exhibits a 97% protein binding rate, and has an elimination half-life of 54 hours. Azelastine, an orally active, selective, and high-affinity histamine H1-receptor antagonist, is utilized in the research of allergic rhinitis, asthma, diabetic hyperlipidemia, and SARS-CoV-2 [1] [2] [3] [4] [5].

H4R antagonist 3 is a novel histamine-4 receptor (H4R) antagonist with an EC50 <10 mM.H4R antagonist 3 has potential inflammatory activity for the study of autoimmune, allergic and ocular diseases.