schizophrenia is a severe psychiatric illness with a lifetime prevalence of ˜1% that imposes a huge toll on patients, their families and public health services worldwide. delusions, hallucinations, disorganized speech, grossly disorganized or catatonic behavior and negative symptoms constitute the core symptoms of schizophrenia. although the neurotransmitter dopamine plays a prominent role in t...

Up to date, there are four pharmacologically characterized subtypes of muscarinic receptors (M1, M2, M3 and M4). In our study we have investigated muscarinic receptor subtypes in smooth muscle layers of human stomach. Isolated preparations of longitudinal and circular muscle layers from human stomach were used. Acetylcholine, bethanechol, carbachol, pilocarpine and AHR -602 produced concen...

Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Acetylcholine Receptors [53]) are activated endogenous agonist acetylcholine. All five (M1-M5) mAChRs ubiquitously expressed in human body and therefore attractive targets for many disorders. Functionally, M1, M3, M5 preferentially couple to Gq/11 proteins, whilst M2 M4 predominantly Gi/o protei...

Muscarinic M2 receptor antagonists with high subtype selectivity (M2/M1) will decrease the toxicity in central nervous system in treatment of AD. The exploration of quantitative structure-selectivity relationship (QSSR) to muscarinic M2 receptor antagonists will provide design information for drug with fewer side effects. In this paper, CoMFA models of pK(i)(M1), pK(i)(M2) and p[K(i)(M2)/K(i)(M...

up to date, there are four pharmacologically characterized subtypes of muscarinic receptors (m1, m2, m3 and m4). in our study we have investigated muscarinic receptor subtypes in smooth muscle layers of human stomach. isolated preparations of longitudinal and circular muscle layers from human stomach were used. acetylcholine, bethanechol, carbachol, pilocarpine and ahr -602 produced concentrati...

Muscarinic acetylcholine receptors belong to a superfamily of structurally related proteins which possess seven transmembrane spanning regions and couple to G-proteins [1-4]. Thus far, five distinct muscarinic receptor subtypes (designated ml-m5) are known to exist based on recent molecular cloning studies [2, 5, 6]. Earlier knowledge of muscarinic receptor heterogeneity was based on binding an...

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...

I The effects of some muscarinic antagonists, namely, N-ethyl-2-pyrrolidylmethyl-cyclopentylphenyl glycollate (PMCG), N-methyl-4-piperidyl-phenylcyclohexyl glycollate (PPCG, racemate and R and S enantiomers) and 4'-N-methyl-piperidyl-1-phenyl-cyclopentane carboxylate (G3063) on organophosphate (sarin, soman)and carbamate (neostigmine)-induced twitch augmentation have been studied in cat soleus ...

Muscarinic blocking drugs are compounds that selectively antagonize the responses to acetylcholine (ACh) and other parasympathomimetics that are mediated by activation of muscarinic receptors. These agents are also referred to as muscarinic antagonists, antimuscarinic drugs, and anticholinergics. The belladonna alkaloids, such as atropine, are the oldest known muscarinic blocking compounds, and...