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Restrict the search for
histamine
to a specific field?
Status:
Possibly Marketed Outside US
Source:
Batebulast hydrochloride
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Batebulast (NCO-650) is an anti-allergic drug. It significantly inhibited both the initial and secondary increases in cAMP stimulated by antigen, anti-IgE and concanavalin A (Con A) in rat peritoneal mast cells. It strongly inhibited the incorporation of the 3H-methyl moiety into phospholipid by antigen, anti-IgE and Con A during histamine release. Batebulast significantly inhibited the compound 48/80-induced bronchoconstriction in dogs. Batebulast had no effect on the bronchoconstriction induced by inhalation of acetylcholine, suggesting that NCO-650 appears to have no anti-cholinergic effect and thus no effect on the vagal reflex that occurred during the asthmatic responses. NCO-650 may be useful for the treatment of bronchial asthma as an orally active drug. Batebulast has been in phase II clinical trials for the treatment of asthma in Japan. However, this research has been discontinued.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pibutidine hydrochloride (IT-066), a novel histamine H2 receptor antagonist has powerful and long lasting antisecretory and antiulcer effects and is a useful antisecretory drug for treatment of peptic ulcer diseases.
Status:
Possibly Marketed Outside US
Source:
Arpromidine by Onbio Inc.
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Arpromidine is a potent histamine H2-receptor agonist and weak NPY Y1 antagonist. In the isolated aperfused heart, arpromidine was more potent in increasing cardiac contractile force and coronary flow but less effective on heart rate and less arrhythmogenic. Arpromidine may be considered a new lead for the development of "cardiohistaminergics". In the arpromidine series the order of potency found in guinea-pig atria was in good agreement with the results from isolated perfused guinea-pig hearts. In particular, the two-fold halogenated arpromidine analogues proved to be more potent positive inotropic agents than impromidine with lower stimulating effects on heart rate and reduced arrhythmogenic properties.
Status:
Possibly Marketed Outside US
Source:
Tiacob by Sanofi-Synthelabo
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. It is used to treat a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. A derivative of benzamide, tiapride is chemically and functionally similar to other benzamide antipsychotics such as sulpiride and amisulpride known for their dopamine antagonist effects. Tiapride is marketed under various trade names and is widely available outside of the United States. The most common trade name for tiapride is Tiapridal, which is used throughout Europe, Russia, as well as parts of South America, the Middle East, and North Africa. It is also sold under different names in Italy (Italprid, Sereprile), Japan (Tialaread, Tiaryl, Tiaprim, Tiaprizal), Chile (Sereprid), Germany (Tiaprid, Tiapridex), and China (Tiapride).
Status:
Possibly Marketed Outside US
Source:
Piprinhydrinate by Kraeber and Co. GmbH
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Piprinhydrinate is compositon of Diphenylpyraline and 8-chloroteophylline. 8-Chlorotheophylline is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine. Diphenylpyraline is an antihistamine that prevents, but does not reverse, responses mediated by histamine alone. Diphenylpyraline antagonizes most of the pharmacological effects of histamine, including urticaria and pruritus. Also, diphenylpyraline may exhibit anticholinergic actions (as do most of the antihistamines) and may thus provide a drying effect on the nasal mucosa. 8-Chlorotheophylline main use is in combination with Diphenylpyraline or diphenhydramine in the antiemetic Piprinhydrinate and dimenhydrinate. Diphenylpyraline (or diphenhydramine) reduces nausea but causes drowsiness, and the stimulant properties of 8-Chlorotheophylline help ward off that side-effect.
Status:
Possibly Marketed Outside US
Source:
Luvistin by Boehringer, Ing.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Histapyrrodine was investigated as a neuro-sedative drug for the treatment of anxiety and states of aggression.
Status:
Possibly Marketed Outside US
Source:
Zepastine by ZYF Pharm Chemical
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Zepastine is antihistamine antiallergic drug developed in the late 1960-s.
Class (Stereo):
CHEMICAL (RACEMIC)
Homochlorcyclizine (INN) is an antihistamine which has been marketed in Japan since 1965. It is used in the treatment of Itching sensation resulting from skin diseases (eczema or dermatitis, pruritus, drug eruption, toxic erythema and infant strophulus), urticaria and allergic rhinitis. Homochlorcyclizine hydrochloride possesses several pharmacological properties: 1) inhibits bradykinin-induced contractions of isolated guinea pig ileum; 2)partially blocks SRS-A (slow-reacting substance of anaphylaxis )- induced contractions in isolated guinea pig il eum. 3) Homochlorcyclizine hydrochloride completely inhibits histamine-induced contractions at a concentration of 0.1μg/mL, while it completely inhibits serotonin or acetylcholine- induced contractions at a concentration of 1μg/mL.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
Sequifenadine is H1- and 5HT-serotonine receptor antagonist. It has an anti-histamine effect, not only blocking histamine receptors, but also reducing the content of histamine in tissues by accelerating its destruction by diamine oxidase. Sequifenadine did not demonstrate any significant sedative effect. It has a pronounced and prolonged antipruritic and antiexudative effect. It is indicated for the treatment of allergic rhinitis and conjunctivitis, pollinosis, urticaria, angioedema, allergic pruritic dermatosis, including atopic dermatitis. Adverse effects are: dry mouth, pain in the epigastric region, dyspepsia, increased appetite, headache, sleepiness.
Status:
Possibly Marketed Outside US
Source:
NCT00622011: Phase 4 Interventional Terminated Delirium
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Zotepine is a potent antipsychotic and antidepressive drug, which was developed in Japan and used in many countries for the treatment of schizophrenia. Zotepine has high affinity to D2, 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, alpha1A, H1, and D1 receptors at therapeutically relevant concentrations and has similar affinities to 5-HT1A, alpha2A, and M1 receptors at high concentrations. In human zotepine is metabolized to a major metabolite, norzotepine, which has profile similar to that of zotepine for important neurotransmitter receptors known to be responsible for zotepine antipsychotic activity.The drug is still available in Asia.
