{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Restrict the search for
histamine
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Eclazolast (REV 2871 or CHBZ) is a non-disodium cromoglycate (DSCG)-like, antiallergic drug. Eclazolast is taken up by rat mast cells and human leukocytes in a specific and saturable manner. The compound can be hydrolyzed by a granule-associated enzyme in the mast cell to an ionic metabolite (REV 3579) whose in vitro profile is identical to that of DSCG. Eclazolast is a potent inhibitor of both immunologic and non-immunologic histamine release. It inhibits exocytosis by intracellularly affecting only direct Fc(epsilon)RI linked processes and not through inhibition of Ca2+ influx channels.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Bavisant (also known as JNJ-31001074 or BEN-2001), a highly selective, active antagonist of the human H3 receptor that was invented by Johnson & Johnson for the treatment of attention-deficit hyperactivity disorder (ADHD). However, the result of clinical trials did not display significant clinical effectiveness in the treatment of adults with ADHD. BenevolentAI has started phase II clinical trials where investigated bavisant for ameliorating the excessive daytime sleepiness in patients with Parkinson’s disease, using one of the drug side effects is dose-dependent insomnia.
Class (Stereo):
CHEMICAL (ACHIRAL)
Metoxepin was developed as an antiemetic, neuroleptic and antihistamine agent. This drug has never been marketed.
Status:
Investigational
Source:
INN:impromidine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Impromidine is a highly potent and specific histamine H2 receptor agonist used diagnostically as a gastric secretion indicator. The value of impromidine as an effective acid-secretory stimulant is limited by its tendency to cause cardiovascular side-effects, that mediated by H2-receptors in the cardiovascular system.
Class (Stereo):
CHEMICAL (RACEMIC)
Piclopastine is an antihistamine agent.
Status:
Investigational
Source:
NCT03441373: Phase 2/Phase 3 Interventional Completed Influenza
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
PF-03893787 is potent and selective histamine H4 receptor (H4R) antagonist. It has comparable binding affinity to the human histamine H3 receptor. PF-03893787 was found to have significant affinity for the hERG channel. Novartis initiates a phase II extension trial in Atopic dermatitis. Studies exploring the utility of PF-3893787 in patients would be reported in due course, being the potential indications of asthma, pruritus, inflammatory skin diseases and pain, among others.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Enerisant is a histamine H3 receptor antagonist. In H3 receptor binding assay using (R)-α-methyl[3H]histamine, enerisant showed IC50 of 4.9 nM. Enerisant may be useful for the treatment of Alzheimer's disease, schizophrenia, etc.
Status:
Investigational
Source:
NCT01493882: Phase 2 Interventional Withdrawn Asthma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
JNJ-39758979 is a histamine H4 receptor antagonist which clinical development for asthma and atopic dermatitis was halted during phase II because of the observation of idiosyncratic drug-induced agranulocytosis in two subjects.
