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Restrict the search for
histamine
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Class (Stereo):
CHEMICAL (ACHIRAL)
Cilutazoline is phenoxymethyl-imidazoline derivative useful as cardiotonics and vasoconstrictors
Class (Stereo):
CHEMICAL (ACHIRAL)
Tuvatidine (HUK 978) is a potent H2-antagonist. HUK 978 was shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors. In both the guinea-pig gastric mucosa preparation and the rat perfused stomach
model, HUK 978 was a powerful inhibitor of acid secretion. HUK 978 is a highly specific H2-antagonist and inhibits acid secretion for longer periods than other competitive compounds.
Class (Stereo):
CHEMICAL (RACEMIC)
FLOTRENIZINE, a diarylmethylpiperazine derivative, is an antihistaminic agent.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Setastine (Loderix) is a potent antagonist of histamine H1-receptor mediated responses. Setastine inhibits anaphylactic shock in guinea-pigs sensitized by horse serum. No antiserotonin, anticholinergic and antiadrenergic effect of the compound can be detected. Setastine has a long lasting (up to 16 h) antihistamine effect with a good oral effectiveness. It shows no cardiovascular effects in cats. Setastine shows a much weaker CNS depressant activity than clemestine fumarate. In displacement studies (3H-mepyramine) setastine had significantly weaker affinity for the central nervous system (CNS) H1-receptors than clemastine fumarate. It is concluded that setastine is a non-sedative highly active H1-antagonist.
Class (Stereo):
CHEMICAL (ACHIRAL)
Ramixotidine (also known as CM 57755 ) is a nicotinamide 1-oxide derivative patented by Sanofi as a gastric antisecretory agent. Ramixotidine is competitive histamine H2-receptor antagonist, that inhibits histamine-induced gastric acid secretion. In preclinical studies, Ramixotidine caused inhibition of dimaprit- or pentagastrin-induced secretion. Acid secretion stimulated by a meat meal was significantly reduced by Ramixotidine Ramixotidine appears to be an inhibitor of gastric acid secretion induced by different stimulants in dogs with a potency comparable to cimetidine. Unfortunately, in clinical trials, Ramixotidine failed to demonstrate efficacy and further development was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Moxastine is a diarylmethane derivative with an antihistamine and anticholinergic activities.
Class (Stereo):
CHEMICAL (ACHIRAL)
ISOCROMIL, a chromone, is an antiallergic agent. It is a mediator release inhibitor used for the treatment of passive cutaneous anaphylaxis and as an anti-asthmatic.
Class (Stereo):
CHEMICAL (ACHIRAL)
Carabestine is the active first-pass metabolite of Ebastine and acts as a histamine H1 receptor antagonist which has been investigated as a potential allergy medication. Ebastine is marketed under a number of brand names.
Class (Stereo):
CHEMICAL (ACHIRAL)
Linetastine has anti-inflammatory and anticarcinogenic effects. It is a potent inhibitor of 5-lipoxygenase. It also inhibits histamine release and epidermal cyclooxygenase activity. It also markedly inhibited TPA-stimulated leukotriene B4 formation, but inhibited formation of prostaglandin E2, a cyclooxygenase product, only slightly. This suggested that neither cyclooxygenase inhibition nor antihistaminic activity were essential to the anti-inflammatory action of linetastine. The anti-inflammatory effect of oral linetastine is probably due to 5-lipoxygenase inhibition. Oral administration of linetastine almost completely suppressed Cyp1a1 mRNA levels in mouse epidermis induced by a topical application of 3-methylcholanthrene or benzo[a]pyrene to mouse skin. Oral administration of linetastine inhibited DMBA-caused skin tumor initiation at least in part by inhibiting Cyp1a1 mRNA induction and epidermal aryl hydrocarbon hydroxylase activity. Linetastine had been in phase II clinical trial for the treatment of allergic rhinitis. However, this study was discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Octasine is an antihistamine agent that has never been marketed.
