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Article: Preclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist - 2nd communication: Lack of central nervous system and cardiovascular effects

TitlePreclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist - 2nd communication: Lack of central nervous system and cardiovascular effects
Authors
Issue Date2000
Citation
Arzneimittel-Forschung/Drug Research, 2000, v. 50 n. 5, p. 441-448 How to Cite?
AbstractDesloratadine (descarboethoxyloratadine, CAS 100643-71-8) is a selective histamine H1 antagonist that exhibits qualitatively similar pharmacodynamic activity to its parent, loratadine (CAS 79794-75-5), but is 2.5-4 times more potent orally. In studies of central nervous system (CNS) effects that might lead to sedation, desloratadine had no behavioral, neurological or autonomic effects in the conscious mouse and rat. At large multiples of the antihistaminic dose in the mouse, it did not inhibit convulsions caused by electroconvulsive shock and inhibited acetic acid-induced writhing only at a dose approximately 1,000 times the antihistaminic dose in the mouse. Desloratadine had no effects on blood pressure, heart rate or electrocardiographic parameters in the rat or guinea pig or on electrocardiographic parameters in the monkey. Notably, there was no effect on the corrected Q-wave to T-wave (QTc) interval. Desloratadine did not inhibit I(Kr) channel human ether-a-go-go-related gene (HERG)-induced current in a study in which HERG was expressed in Xenopus oocytes. In the rat, desloratadine did not cause effects in urine volume, electrolytes or creatinine, or inhibit gastric emptying or intestinal transit, or cause any harmful effects on gastric mucosa. The results of these preclinical studies provide evidence that desloratadine is a safe antihistamine without CNS or cardiovascular effects.
Persistent Identifierhttp://hdl.handle.net/10722/170026
ISSN
2014 Impact Factor: 0.701
2015 SCImago Journal Rankings: 0.212
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorKreutner, Wen_US
dc.contributor.authorHey, JAen_US
dc.contributor.authorChiu, Pen_US
dc.contributor.authorBarnett, Aen_US
dc.date.accessioned2012-10-30T06:04:49Z-
dc.date.available2012-10-30T06:04:49Z-
dc.date.issued2000en_US
dc.identifier.citationArzneimittel-Forschung/Drug Research, 2000, v. 50 n. 5, p. 441-448en_US
dc.identifier.issn0004-4172en_US
dc.identifier.urihttp://hdl.handle.net/10722/170026-
dc.description.abstractDesloratadine (descarboethoxyloratadine, CAS 100643-71-8) is a selective histamine H1 antagonist that exhibits qualitatively similar pharmacodynamic activity to its parent, loratadine (CAS 79794-75-5), but is 2.5-4 times more potent orally. In studies of central nervous system (CNS) effects that might lead to sedation, desloratadine had no behavioral, neurological or autonomic effects in the conscious mouse and rat. At large multiples of the antihistaminic dose in the mouse, it did not inhibit convulsions caused by electroconvulsive shock and inhibited acetic acid-induced writhing only at a dose approximately 1,000 times the antihistaminic dose in the mouse. Desloratadine had no effects on blood pressure, heart rate or electrocardiographic parameters in the rat or guinea pig or on electrocardiographic parameters in the monkey. Notably, there was no effect on the corrected Q-wave to T-wave (QTc) interval. Desloratadine did not inhibit I(Kr) channel human ether-a-go-go-related gene (HERG)-induced current in a study in which HERG was expressed in Xenopus oocytes. In the rat, desloratadine did not cause effects in urine volume, electrolytes or creatinine, or inhibit gastric emptying or intestinal transit, or cause any harmful effects on gastric mucosa. The results of these preclinical studies provide evidence that desloratadine is a safe antihistamine without CNS or cardiovascular effects.en_US
dc.languageengen_US
dc.relation.ispartofArzneimittel-Forschung/Drug Researchen_US
dc.subject.meshAnimalsen_US
dc.subject.meshAnticonvulsants - Pharmacologyen_US
dc.subject.meshAutonomic Nervous System - Drug Effectsen_US
dc.subject.meshBehavior, Animal - Drug Effectsen_US
dc.subject.meshCardiovascular System - Drug Effectsen_US
dc.subject.meshCentral Nervous System - Drug Effectsen_US
dc.subject.meshDigestive System - Drug Effectsen_US
dc.subject.meshGuinea Pigsen_US
dc.subject.meshHemodynamics - Drug Effectsen_US
dc.subject.meshHistamine H1 Antagonists - Pharmacologyen_US
dc.subject.meshKidney - Drug Effectsen_US
dc.subject.meshLoratadine - Analogs & Derivatives - Pharmacologyen_US
dc.subject.meshMacaca Fascicularisen_US
dc.subject.meshMaleen_US
dc.subject.meshMiceen_US
dc.subject.meshRatsen_US
dc.titlePreclinical pharmacology of desloratadine, a selective and nonsedating histamine H1 receptor antagonist - 2nd communication: Lack of central nervous system and cardiovascular effectsen_US
dc.typeArticleen_US
dc.identifier.emailChiu, P:pkychiu@hkucc.hku.hken_US
dc.identifier.authorityChiu, P=rp00379en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.pmid10858871-
dc.identifier.scopuseid_2-s2.0-0034111253en_US
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0034111253&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume50en_US
dc.identifier.issue5en_US
dc.identifier.spage441en_US
dc.identifier.epage448en_US
dc.identifier.isiWOS:000087503600004-
dc.identifier.scopusauthoridKreutner, W=7006681605en_US
dc.identifier.scopusauthoridHey, JA=7102045551en_US
dc.identifier.scopusauthoridChiu, P=7202988127en_US
dc.identifier.scopusauthoridBarnett, A=24572200500en_US

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