Drugs online research references
Arch Int Pharmacodyn Ther. 1986 Apr;280(2):275-91.
Comparative study of various H1-blockers on neuropharmacological and behavioral effects including 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole difumarate (KB-2413), a new antiallergic agent.
Tasaka K, Kamei C, Katayama S, Kitazumi K, Akahori H, Hokonohara T.
In a conditioned avoidance response tested in rats, all of the H1-blockers employed caused a dose-related inhibition at doses 5-20 mg/kg (i.v.) except for ketotifen that elicited significant suppression even at a dose of 1 mg/kg. No inhibition was seen after administration of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole difumarate (KB-2413). ED50s were ranged from 4.1 to 7.4 mg/kg in diphenhydramine, pyrilamine and promethazine. In laminectomized rats, diphenhydramine, pyrilamine, promethazine and ketotifen suppressed the amplitudes of monosynaptic reflex potentials at doses higher than 2 mg/kg (i.v.). In the case of chlorpheniramine, significant inhibition was observed at a dose of 20 mg/kg. In a polysynaptic reflex, similar but less prominent inhibitions were affected by those drugs. However, KB-2413 did not influence spinal reflexes even at a dose of 20 mg/kg. In the rat phrenic nerve-diaphragm preparation, perfusion of H1-blockers at a concentration of 10(-5) M decreased the amplitudes of end-plate potentials except for chlorpheniramine and KB-2413. At 10(-4) M, all the test drugs caused significant inhibition. When the action potential of superior cervical ganglion was measured by the sucrose gap method, promethazine inhibited the action potential significantly at 10(-6) M, but the rest of the test drugs depressed the potentials at 10(-5) M. In spontaneous EEG, all H1-blockers caused a marked drowsy pattern at lower doses (2-5 mg/kg) except for chlorpheniramine, while in higher doses (10-20 mg/kg) epileptic signs in EEG with or without convulsive behavior were noticed. However, after KB-2413 (5-20 mg/kg) neither drowsy nor seizure pattern was observed, in EEG or behavior.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2872864&dopt=Abstract
Pharmacol Toxicol. 1987 Feb;60(2):100-3.
Antibacterial effect of four phenothiazines.
Kristiansen JE, Mortensen I.
Various types of phenothiazines were examined for antibacterial effect on 61 Gram-positive and Gram-negative bacterial strains in vitro. The investigated phenothiazines were two neuroleptic drugs, fluphenazine and chlorpromazine, and two antihistaminic drugs, alimemazine and promethazine. All four drugs have antibacterial effects in vitro, the phenothiazines being more potent against the Gram-positive microorganisms. The antibacterial potency of the drugs was measured as IC50: Fluphenazine 29 microM (15 micrograms/ml), alimemzaine 49 microM (37 micrograms/ml), promethazine 88 microM (28 micrograms/ml) and chlorpromazine 92 microM (29 micrograms/ml). The antibacterial potency of the drugs was linked neither to the neuroleptic nor the antihistaminic potency of the drugs, which is in agreement with results of earlier stereoisomeric investigations. Thus, the known phenothiazines may represent a pool of potentially new antimicrobial drugs. A therapeutic application of these results, however, requires additional in vitro an in vivo testing in an animal model. The bacterial model might be of value as a model system in the study of the interaction of neuropharmacological agents and other membrane active compounds on biological membranes.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2883644&dopt=Abstract
Rhinology. 1987 Jun;25(2):95-100.
Effects of H1 antihistamines on canine nasal vascular and airway resistances.
Lung MA, Wang JC.
The effects of three commonly used H1 antihistamines on the nasal vascular and airway resistances were studied in the dog. Promethazine hydrochloride decreased nasal vascular resistance but increased nasal airway resistance in a dose-dependent manner. Diphenylpyraline hydrochloride in low doses increased nasal vascular resistance without affecting much nasal airway resistance while in high doses decreased nasal vascular resistance but increased nasal airway resistance. Chlorpheniramine maleate in low doses increased nasal vascular resistance but decreased nasal airway resistance while in high doses decreased nasal vascular resistance without affecting much nasal airway resistance. It was concluded that different H1 antihistamines might exert vasoconstrictor or vasodilatatory action on both the resistance and capacitance vessels of the nasal vascular bed depending on the type and the dose of the drug used.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2887028&dopt=Abstract
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