Histamine H receptor antagonists,

Bakker, R. A., Wieland, K., Timmerman, H. and Leurs, R. Constitutive activity of the histamine H[ receptor reveals inverse agonism of histamine H receptor antagonists. Eur. J. Pharmacol. 387 R5-R7, 2000. 

Interestingly, penicillamine—a degradation product of penicillin and phenothiazines—the histamine H,—receptor antagonists, such as promethazine teoclate, methadilazine hydrochloride, trimeprazine tartrate are found to increase the cholesterol levels. 

An interesting observation in our structure-activity studies was that ethylamine, a part of the histamine molecule, 4-(2-ethylamine)imidazole, known for a long time to be a potent stimulator of gastric secretion, also produced duodenal ulcers in rats (20,22). Furthermore, structural similarities also exist between dopamine and histamine H receptor antagonists metiamide and cimetidine (23,24). 

Zhang MQ, Leurs R, Timmerman H. Histamine H receptor antagonists. In Burger s Medicinal Chemistry and Drug Discovery. Wolff M E (Ed.).)ohn Wiley Sons, 1997. 

Buclizirte hydrochloride is (RS)-l-(4-ferf-butylbenzyl)-4-(4-chlorober zhy-dryl)piperazir e dihydrochloride. It contains not less than 99% and not more than 100.5% of C28H33C1N2-2HC1, calculated with reference to the dried substance. It is a histamine H-receptor antagonist and antiemetic. 

Histamine H -receptor antagonists cimetidine, famotidine, nizatidine, ranitidine (see Ch. 31). 

The goals of PUD therapy are to promote healing, relieve pain, and prevent ulcer complications and recurrences. Medications used to heal or reduce ulcer recurrence include antacids. histamine H -receptor antagonists, protective mucosal barriers, proton pump inhibitors, prostaglandins, and bismuth salt and antibiotic combinations. 

Clebopride malate clebopride, clemastine [ban, inn, usan] (clemastine fumarate [jan, usan] Aller-eze Tavegil Tavist ) is a methylpyrrolidine, a histamine h,-RECEPTOR ANTAGONIST, with some MUSCARINIC CHOLINOCEPTOR ANTAGONIST and SEDATIVE activity. It can be used orally for the symptomatic relief of allergic symptoms, such as hay fever and urticaria. Clemastine fumarate clemastine. 

Cyclimorph cyclizlne tartrate morphine tartrate, cyclizine [ban, inn) (cyclizIne hydrochloride (usan) cyclizlne tartrate BW 47-83 Valoid ) is one of the piperazine series of histamine H -receptor ANTAGONISTS, and a muscarinic CHOLINOCEPTOR antagonist with SEDATIVE actions. It can be used orally or systemically as an antiemetic in the treatment of nausea, vomiting, vertigo, motion sickness and disorders of the balance function of the inner ear. It is available in preparation together with morphine (e.g. Cyclimorph ). 

At least two receptors have been cloned. These include NTSl (NTR-1 NTl high-affinity neurotensin receptor) at which the synthetic peptide analogue JMV449 is selective, and nts2 (where the functional relevance is yet to be elucidated) and here levocabastine, a histamine H] receptor antagonist, has a reasonably high affinity. 

ANTIBACTERICAL, ANTIFUNGAL, antifungicide and ANTIVIRAL properties. It can be used as a vapour and is rather toxic, propiomazine [ban, inn, usan] (propiomazine hydrochloride [usan] propiomazine maleate Wy 1359 Propavan ) is a phenothiazine with HISTAMINE H -RECEPTOR ANTAGONIST properties, but is used as a SEDATIVE, a HYPNOTIC and in preoperative medication, propiomazine hydrochloride propiomazine. propiomazine maleate propiomazine. propiram [ban, inn] (propiram fumarate [usan] Bay 4503) is one of the phenylpiperidine series, an opioid RECEPTOR AGONIST with OPIOID ANALGESIC activity. 

Loratadine. 4 i8-Chloro-Sf6-dihydro-l lH bettzo [bjcyctoh epta[I, 2 bJpyridi n -11 -y f i den e) t-p f peri di n cca rb-oxylic acid ethyl ester ll-l/V- ethoxycarbonyl)-4-piperidyl-idene]-8-chlorO-6,l l -dihydrO-Sif-benzo cyclohepta-tl 2-6]pyridine Sch-29851 Clantin CLaritin Clarityne Lisino. C HjjClNjOji mol wt 3 2.89. C 69 01%, H 6,05%, Cl 9 26%, N 7-32%, O 8.36%. Nonsedating-type histamine H.-receptor antagonist. Prepn F. J. Vtllani, U.S. pat. 

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