Tolterodine and its Active 5-Hydroxymethyl Metabolite: Pure Muscarinic Receptor Antagonists
نویسندگان
چکیده
منابع مشابه
[Selective muscarinic receptor antagonists].
3ubtypes of muscarmic receptors, first hypothesized by Birdsall et al. ~ to explain the anomalous binding of cholinergic agonists to brain receptors~ were later demonstrated with the seEective muscarinic antagonist, pirenzepine 2. Interestingly, the search for selective antagonists, which usually follows the acceptance of a concept, antedated by many years the notion of heterogeneity of rmecari...
متن کاملMuscarinic Receptor Agonists and Antagonists
A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the treatment of Alzheimer’s disease are discussed. A selection of chemical routes are described, which illustrate contemporary methodology for the synthes...
متن کاملCharacterization of Muscarinic Receptor Binding of Fesoterodine after Oral Administration in Rats
Hypothesis / aims of study Fesoterodine is a relatively novel antimuscarinic agent for the treatment of overactive bladder (OAB) [1]. When administered orally, fesoterodine is rapidly and extensively converted to its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), which is also an active metabolite of tolterodine [2]. Our recent study with radioligand binding assay has shown that fesote...
متن کاملDevelopment of pure prolactin receptor antagonists.
Prolactin (PRL) promotes tumor growth in various experimental models and leads to prostate hyperplasia and mammary neoplasia in PRL transgenic mice. Increasing experimental evidence argues for the involvement of autocrine PRL in this process. PRL receptor antagonists have been developed to counteract these undesired proliferative actions of PRL. However, all forms of PRL receptor antagonists ob...
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ژورنال
عنوان ژورنال: Pharmacology & Toxicology
سال: 2002
ISSN: 0901-9928
DOI: 10.1034/j.1600-0773.2002.900506.x