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Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).
Competition experiments with [(3)H]mepyramine showed that cetirizine and its enantiomers, levocetirizine and (S)-cetirizine, bound with high affinity and stereoselectivity to human H(1) histamineExpand
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Binding characteristics of [3H]ucb 30889 to levetiracetam binding sites in rat brain.
Levetiracetam (2S-(2-oxo-1-pyrrolidinyl)butanamide, KEPPRA, a novel antiepileptic drug, has been shown to bind to a specific binding site located in brain (levetiracetam binding site [Eur. J.Expand
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BRAIN DISTRIBUTION OF CETIRIZINE ENANTIOMERS: COMPARISON OF THREE DIFFERENT TISSUE-TO-PLASMA PARTITION COEFFICIENTS: Kp, Kp,u, AND Kp,uu
The objective of this study was to compare the blood-brain barrier (BBB) transport and brain distribution of levo- (R-CZE) and dextrocetirizine (S-CZE). Microdialysis probes, calibrated usingExpand
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Recent Developments In Noradrenergic Neurotransmission and its Relevance to the Mechanism of Action of Certain Antihypertensive Agents
SUMMARY This report reviews a number of significant developments in the fields of noradrenergic transmission and adrenergic receptors which suggest that, hi addition to the classical postsynapticExpand
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THE PHARMACOLOGY OF ANTIHYPERTENSIVE DRUGS WITH SPECIAL REFERENCE TO VASODILATORS, α‐ADRENERGIC BLOCKING AGENTS AND PRAZOSIN
Prazosin causes relaxation of vascular smooth muscle and produces a non‐classical functional blockade of α‐adrenoceptors quite unlike the occupancy block caused by conventional α‐adrenoceptorExpand
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Pre- and postsynaptic alpha adrenoceptor selectivity studies with yohimbine and its two diastereoisomers rauwolscine and corynanthine in the anesthetized dog.
The selectivity of yohimbine and its two diastereoisomers rauwolscine and corynanthine for pre- and postsynaptic alpha adrenoceptors has been investigated in the anesthetized dog. Antagonism of theExpand
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A comparsion of the effects of prazosin and hydrallazine on blood pressure, heart rate and plasma renin activity in conscious renal hypertensive dogs.
Prazosin, a novel antihypertensive agent, and hydrallazine have been compared in renal hypertensive dogs. I.v. prazosin (0.1 mg/kg) produced greater falls in blood pressure than hydrallazine (1 mg/kgExpand
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In vivo selectivity of prazosin but not of WB4101 for postsynaptic alpha-1 adrenoceptors.
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Stereoselective pharmacokinetics of cetirizine in the guinea pig: role of protein binding
Purpose. To characterize the pharmacokinetics of cetirizine enantiomers in the guinea pig including protein binding in both the guinea pig and human plasma.
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Binding characteristics of [3H]levocetirizine to cloned human H1-histamine-receptors expressed in CHO cells
Cetirizine (ZyrtecTM) and levocetirizine (XyzalTM) are second generation antihistamines prescribed for perennial rhinitis and urticaria. Both drugs display nanomolar affinity towardsExpand
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