U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 131 - 140 of 1608 results

Status:
Investigational
Source:
INN:quisultazine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Quisultazine is a phenothiazine derivative patented by MARPHA Societe d'Etude et d'Exploitation de Marques as pentagastrin antagonist. In preclinical studies, Quisultazine weakly inhibited pentagastrin-stimulated gastric secretion but was a powerful inhibitor of nocturnal gastric secretion. Quisultazine possesses a very weak affinity to muscarinic receptors in vitro and in vivo. It has negligible anticholinergic properties in rats and mice at the peripheral level but no effect at the central level.
Status:
Investigational
Source:
INN:cipralisant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cipralisant (GT-2331) is an H3-receptor ligand developed by Gliatech in the late 1990s. The drug exhibits complex pharmacology: it behaves as an antagonist in a guinea pig jejunum contraction assay and mouse disogenia model, as a partial agonist in a rat brain synaptosome model, and as a full agonist at recombinant H3 receptors. In preclinical models, cipralisant enhanced wakefulness and improved learning in developmental rat models. In 2000 cipralisant was investigated in the clinical trials for the treatment of attention-deficit hyperactivity disorder, but due to the bankruptcy of Gliatech the development of the drug was discontinued.
Status:
Investigational
Source:
INN:vapitadine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Vapitadine (R129160; Hivenyl™) is an antihistamine that Barrier Therapeutics is developing as a treatment for allergic reactions of the skin, such as those associated with hives and for the itch associated with atopic dermatitis. Vapitadine is a new selective, non-sedative H1antihistamine. In several in vitro and in vivo pharmacological models, vapitadine is at least as potent as cetirizine (Zyrtec®) and does not penetrate the blood-brain barrier. An advantage of vapitadine over other antihistamines may be the absence of the sedation, even at high doses. Vapitadine had been in phase II clinical trials for the treatment of patients with atopic dermatitis. However, no development has been reported.
Status:
Investigational
Source:
INN:lamtidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LAMTIDINE is an irreversible and specific gastric histamine H2-receptor antagonist.
Status:
Investigational
Source:
INN:clobenzepam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Clobenzepam (tarpane) is a drug exhibiting antihistaminic properties.
Status:
Investigational
Source:
INN:dorastine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

There is no information about biological and medical application of dorastine . It’s known, that compound possesses antihistamine properties and can be obtained from 4-chloroaniline.
Status:
Investigational
Source:
INN:pirdonium bromide
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Pirdonium is an antihistamine agent. It is the hydrophilic Histamine H1 receptor antagonist.
Status:
Investigational
Source:
INN:propinetidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Propinetidine is a piperidinol derivative patented by Farbenfabriken Bayer Akt.-Ges. as antitussive agent.
Status:
Investigational
Source:
NCT01006122: Phase 2 Interventional Completed Excessive Daytime Sleepiness
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PF-03654746 is a potent, selective antagonist of the human H3 receptor, developed by Pfizer. It was in the clinical trial phase II for the treatment of excessive daytime sleepiness (EDS) associated with narcolepsy, Tourette syndrome as well as potential anti-allergy applications and in phase I of clinical trial for the treatment of Schizophrenia and Alzheimer's disease, but these investigations were discontinued.
Status:
Investigational
Source:
INN:irdabisant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

IRDABISANT is a histamine H3 receptor inverse agonist with potential therapeutic utility in cognition enhancement.