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- Publications
- Influence
Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).
- M. Gillard, C. Van der Perren, N. Moguilevsky, R. Massingham, P. Chatelain
- Chemistry, Medicine
- Molecular pharmacology
- 1 February 2002
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) histamine… Expand
Binding characteristics of [3H]ucb 30889 to levetiracetam binding sites in rat brain.
- M. Gillard, B. Fuks, P. Michel, P. Vertongen, R. Massingham, P. Chatelain
- Chemistry, Medicine
- European journal of pharmacology
- 30 September 2003
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
BRAIN DISTRIBUTION OF CETIRIZINE ENANTIOMERS: COMPARISON OF THREE DIFFERENT TISSUE-TO-PLASMA PARTITION COEFFICIENTS: Kp, Kp,u, AND Kp,uu
- Anubha Gupta, P. Chatelain, R. Massingham, E. Jonsson, M. Hammarlund-Udenaes
- Chemistry, Medicine
- Drug Metabolism and Disposition
- 1 February 2006
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 using… Expand
Recent Developments In Noradrenergic Neurotransmission and its Relevance to the Mechanism of Action of Certain Antihypertensive Agents
- S. Langer, I. Cavero, R. Massingham
- Chemistry, Medicine
- Hypertension
- 1 July 1980
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 postsynaptic… Expand
THE PHARMACOLOGY OF ANTIHYPERTENSIVE DRUGS WITH SPECIAL REFERENCE TO VASODILATORS, α‐ADRENERGIC BLOCKING AGENTS AND PRAZOSIN
- D. Cambridge, M. Davey, R. Massingham
- Medicine
- The Medical journal of Australia
- 1 August 1977
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‐adrenoceptor… Expand
Pre- and postsynaptic alpha adrenoceptor selectivity studies with yohimbine and its two diastereoisomers rauwolscine and corynanthine in the anesthetized dog.
- N. Shepperson, N. Duval, R. Massingham, S. Langer
- Chemistry, Medicine
- The Journal of pharmacology and experimental…
- 1 November 1981
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 the… Expand
A comparsion of the effects of prazosin and hydrallazine on blood pressure, heart rate and plasma renin activity in conscious renal hypertensive dogs.
- R. Massingham, M. L. Hayden
- Medicine
- European journal of pharmacology
- 1975
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/kg… Expand
In vivo selectivity of prazosin but not of WB4101 for postsynaptic alpha-1 adrenoceptors.
- R. Massingham, M. Dubocovich, N. Shepperson, S. Langer
- Chemistry, Medicine
- The Journal of pharmacology and experimental…
- 1 May 1981
Stereoselective pharmacokinetics of cetirizine in the guinea pig: role of protein binding
- Anubha Gupta, M. Hammarlund-Udenaes, P. Chatelain, R. Massingham, E. Jonsson
- Chemistry, Medicine
- Biopharmaceutics & drug disposition
- 1 September 2006
Purpose. To characterize the pharmacokinetics of cetirizine enantiomers in the guinea pig including protein binding in both the guinea pig and human plasma.
Binding characteristics of [3H]levocetirizine to cloned human H1-histamine-receptors expressed in CHO cells
- M. Gillard, C. Van der Perren, R. Massingham, P. Chatelain
- Chemistry, Medicine
- Inflammation Research
- 1 April 2002
Cetirizine (ZyrtecTM) and levocetirizine (XyzalTM) are second generation antihistamines prescribed for perennial rhinitis and urticaria. Both drugs display nanomolar affinity towards… Expand