Histamine Receptor

Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant, which is an orally active, effective, selective and high-affinity histamine H3 receptor antagonist (rat Ki=0.47 nM).

Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, effective, selective and high-affinity antagonist of the histamine H3 receptor in vivo. In vitro, it acts as an agonist of the histamine H3 receptor with a pKi value of 9.9 and a Ki value of 0.47 nM for rat histamine H3 receptors. Cipralisant (maleate) has potential in research on attention deficit hyperactivity disorder.

Diphenhydramine-d5 (hydrochloride) is the deuterated form of Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation antihistamine with anticholinergic properties that acts as an antagonist at histamine H1-receptors. It can cross the blood-brain barrier.

Diphenhydramine-d6 (hydrochloride) is the deuterated form of Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation antihistamine with anticholinergic properties that acts as an antagonist at histamine H1-receptors. It can cross the blood-brain barrier.

Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier permeable antagonist/inverse agonist of the histamine H3 receptor (H3R), with Ki values of 7.2 nM for rat H3R and 2.0 nM for human H3R. Irdabisant has relatively low inhibitory activity on hERG currents, with an IC50 value of 13.8 μM. In rat social cognition models, Irdabisant has cognitive enhancing and arousal effects. Irdabisant can be used in research related to schizophrenia or cognitive impairment.

Promethazine-d4 (hydrochloride) is the deuterated form of Promethazine hydrochloride. Promethazine hydrochloride is a first-generation antihistamine with H1 receptor potent antagonism and mAChR antagonism, as well as some affinity for 5-HT2A, 5-HT2C, D2, and alpha-1 adrenergic receptors.

(R)-(+)-Dimethindene maleate is an orally active H1-receptor blocker with anti-histamine properties in pigs.

Repirinast (MY-5116) is an orally active anti-allergic agent.

ST-1006 is a potent histamine H4 receptor agonist with a pKi value of 7.94.

Histamine H4 receptor antagonist-1 is an antagonist of histamine H4 receptor extracted from patent WO2010108059A1 compound 60.

Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.

H3R-IN-1 is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.

(S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent antagonist of H1 receptor-mediated responses.

Enerisant is a potent, selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors.

BMY-25368 drochloride is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor.

Spinacetin is a natural product that can be isolated from Inula japonica.

Betazole hydrochloride (Ametazole hydrochloride), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist.

(R)-(-)-Chlorpheniramine maleate is an enantiomer of Chlorpheniramine maleate.

BP1.3656B is a selective, orally active, blood-brain barrier-permeable histamine H3 receptor ( histamine H3 receptor ) inverse agonist/antagonist, with a K B value of 0.08 nM for antagonizing agonist-induced activity and an IC 50 value of 0.38 nM for directly inhibiting the basal activity of the receptor.

PIPE-791 is an orally active, blood-brain barrier-permeable selective antagonist of LPAR1.

N-Desmethyl xanomeline is a pharmacologically active metabolite of Xanomeline.

histamine H1-receptor antagonist