Literature DB >> 8257954

Terfenadine: a mixture of equipotent antihistamine enantiomers without a clear 'isomeric ballast'.

M Q Zhang1, H Timmerman.   

Abstract

Terfenadine was the first non-sedating histamine H1 receptor antagonist and one of the most frequently prescribed H1 antihistamines. Terfenadine has one asymmetric centre in the molecule and is currently used as a racemate. Different methods and approaches for obtaining pure enantiomers of terfenadine are summarized and discussed in the present paper. Studies on antihistamine activity of the enantiomers, their side-effects on the central nervous system, calcium channel affinity and metabolism are also reviewed and analysed.

Entities:  

Mesh：

Substances：

Year:  1993        PMID： 8257954     DOI： 10.1007/bf01880624

Source DB:  PubMed          Journal:  Pharm World Sci        ISSN： 0928-1231


  15 in total

1.  Torsades de Pointes after treatment with terfenadine and ketoconazole.

Authors:  M Zimmermann; H Duruz; O Guinand; O Broccard; P Levy; D Lacatis; A Bloch
Journal:  Eur Heart J       Date:  1992-07       Impact factor: 29.983

2.  Determination of the metabolites of terfenadine in human urine by thermospray liquid chromatography-mass spectrometry.

Authors:  T M Chen; K Y Chan; J E Coutant; R A Okerholm
Journal:  J Pharm Biomed Anal       Date:  1991       Impact factor: 3.935

3.  Mode of action of calcium antagonists on responses to spasmogens and antigen challenge in human airway smooth muscle.

Authors:  M S Kannan; C Davis
Journal:  Respir Physiol       Date:  1988-10

4.  Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.

Authors:  R C Young; R C Mitchell; T H Brown; C R Ganellin; R Griffiths; M Jones; K K Rana; D Saunders; I R Smith; N E Sore
Journal:  J Med Chem       Date:  1988-03       Impact factor: 7.446

5.  Is there a difference in the affinity of histamine H1 receptor antagonists for CNS and peripheral receptors? An in vitro study.

Authors:  A M Ter Laak; G M Donné-Op den Kelder; A Bast; H Timmerman
Journal:  Eur J Pharmacol       Date:  1993-03-02       Impact factor: 4.432

6.  Chiral manipulation of drug selectivity: studies on a series of terfenadine-derived dual antagonists on H1-receptors and calcium channels.

Authors:  M Q Zhang; P Caldirola; H Timmerman
Journal:  Agents Actions       Date:  1994-06

7.  Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacology.

Authors:  E J Ariëns
Journal:  Eur J Clin Pharmacol       Date:  1984       Impact factor: 2.953

8.  Relationship between occupation of cerebral H1-receptors and sedative properties of antihistamines. Assessment in the case of terfenadine.

Authors:  C Rose; T T Quach; C Llorens; J C Schwartz
Journal:  Arzneimittelforschung       Date:  1982

Review 9.  Terfenadine. An updated review of its pharmacological properties and therapeutic efficacy.

Authors:  D McTavish; K L Goa; M Ferrill
Journal:  Drugs       Date:  1990-04       Impact factor: 9.546

10.  Direct enantiomeric separation of terfenadine and its major acid metabolite by high-performance liquid chromatography, and the lack of stereoselective terfenadine enantiomer biotransformation in man.

Authors:  K Y Chan; R C George; T M Chen; R A Okerholm
Journal:  J Chromatogr       Date:  1991-11-15
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.