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British Journal of Pharmacology Aug 19881. The affinity of the antagonist dicyclomine for subtypes of muscarinic receptors has been assessed in the myenteric plexus-longitudinal muscle preparation of the...
1. The affinity of the antagonist dicyclomine for subtypes of muscarinic receptors has been assessed in the myenteric plexus-longitudinal muscle preparation of the guinea-pig. 2. Dicyclomine had a high affinity (pA2 9.13) for the neuronal M1-receptor whose activation by pilocarpine causes an increase in acetylcholine release. Dicyclomine had a low affinity for both the prejunctional M2-receptor (pA2 7.61) mediating inhibition of the electrically-evoked acetylcholine release and the postjunctional M2-receptor (pA2 7.21). 3. It is concluded that dicyclomine distinguishes between M1- and M2-muscarinic receptors in functional experiments.
Topics: Animals; Cyclohexanecarboxylic Acids; Dicyclomine; Electric Stimulation; Guinea Pigs; Ileum; In Vitro Techniques; Muscle Contraction; Muscle, Smooth; Oxotremorine; Receptors, Muscarinic
PubMed: 3207984
DOI: 10.1111/j.1476-5381.1988.tb11647.x -
Physiology & Behavior Feb 2017Several studies have investigated the transition of consolidation of recent memory to remote memory in aversively motivated tasks, such as contextual fear conditioning...
Several studies have investigated the transition of consolidation of recent memory to remote memory in aversively motivated tasks, such as contextual fear conditioning (CFC) and inhibitory avoidance (IA). However, the mechanisms that serve the retrieval of remote memories, has not yet been fully understood. Some evidences suggest that the central cholinergic system appears be involved in the modulation of these processes. Therefore, the present study aimed to investigate the effects of a pre-test administration of dicyclomine, a high-affinity M1 muscarinic receptor antagonist, on the retrieval of remote memories in fear conditioning and IA tasks. Male Wistar rats were trained, and after 1 or 28days, the rats received dicyclomine (16 or 32mg/kg, intraperitoneally, i.p.) and were tested in CFC, tone fear conditioning (TFC) and IA tasks. At both time intervals, 32mg/kg dicyclomine induced impairment of CFC. In TFC task only the performance of the rats 28days after training was impaired. The IA task was not affected in any of the studied intervals. These findings suggest a differential contribution of muscarinic receptors on recent and remote memories retrieval revealing a more generalized role in remote memory.
Topics: Acoustic Stimulation; Analysis of Variance; Animals; Avoidance Learning; Conditioning, Classical; Dicyclomine; Dose-Response Relationship, Drug; Fear; Male; Mental Recall; Muscarinic Antagonists; Rats; Rats, Wistar; Receptor, Muscarinic M1; Time Factors
PubMed: 27940145
DOI: 10.1016/j.physbeh.2016.12.008 -
Molecules (Basel, Switzerland) Oct 2018The Emerald Ash Borer (EAB), , Fairmaire, an Asian invasive alien buprestid has devastated tens of millions of ash trees ( spp.) in North America. Foliar phytochemicals...
The Emerald Ash Borer (EAB), , Fairmaire, an Asian invasive alien buprestid has devastated tens of millions of ash trees ( spp.) in North America. Foliar phytochemicals of the genus (Oleaceae): (Green ash), (White ash), (Bush) Bush. (Pumpkin ash), Michx. (Blue ash), Marsh. (Black ash) and . (Manchurian ash) were investigated using HPLC-MS/MS and untargeted metabolomics. HPLC-MS/MS help identified 26 compounds, including phenolics, flavonoids and coumarins in varying amounts. Hydroxycoumarins, esculetin, esculin, fraxetin, fraxin, fraxidin and scopoletin were isolated from blue, black and Manchurian ashes. High-throughput metabolomics revealed 35 metabolites, including terpenes, secoiridoids and lignans. Metabolomic profiling indicated several upregulated putative compounds from Manchurian ash, especially fraxinol, ligstroside, oleuropin, matairesinol, pinoresinol glucoside, 8-hydroxypinoresinol-4-glucoside, verbenalin, hydroxytyrosol-1--glucoside, totarol and ar-artemisene. Further, dicyclomine, aphidicolin, parthenolide, famciclovir, ar-turmerone and myriocin were identified upregulated in blue ash. Principal component analysis demonstrated a clear separation between Manchurian and blue ashes from black, green, white and pumpkin ashes. The presence of defensive compounds upregulated in Manchurian ash, suggests their potential role in providing constitutive resistance to EAB, and reflects its co-evolutionary history with , where they appear to coexist in their native habitats.
Topics: Animals; Chromatography, High Pressure Liquid; Coleoptera; Coumarins; Flavonoids; Fraxinus; Metabolome; Metabolomics; Molecular Structure; Phenols; Tandem Mass Spectrometry
PubMed: 30360500
DOI: 10.3390/molecules23112734 -
British Journal of Pharmacology Jan 19921. The ability to modify the pain threshold by the two M1-muscarinic agonists: McN-A-343 and AF-102B and by the specific M2-agonist arecaidine was examined in mice and...
1. The ability to modify the pain threshold by the two M1-muscarinic agonists: McN-A-343 and AF-102B and by the specific M2-agonist arecaidine was examined in mice and rats by using three different noxious stimuli: chemical (writhing test), thermic (hot-plate test) and mechanical (paw pressure test). 2. In the mouse hot-plate test McN-A-343 (20-50 micrograms per mouse i.c.v.) and AF-102B (1-10 mg kg-1 i.p.) produced significant antinociception which was prevented by atropine (1 microgram per mouse i.c.v.) and by the two selective M1 antagonists: pirenzepine (0.01 micrograms per mouse i.c.v.) and dicyclomine (0.08 micrograms per mouse i.c.v. or 10 mg kg-1 i.p.) but not by the specific M2-antagonist AFDX-116 (0.1 micrograms per mouse i.c.v.), naloxone (1 mg kg-1 i.p.) or by the acetylcholine (ACh) depletor hemicholinium-3 (HC-3) (1 micrograms per mouse i.c.v.). McN-A-343 and AF-102B were able to increase the pain threshold also in the mouse acetic acid writhing test and in rat paw pressure test. These antinociceptive effects were completely prevented by dicyclomine (0.08 micrograms per mouse i.c.v. or 10 mg kg-1 i.p.) but not by AFDX-116 (0.1 microgram per mouse or rat i.c.v.). 3. In contrast with the M1-agonists, the M2-agonist arecaidine (0.1-2 micrograms per mouse or rat i.c.v.) did not induce antinociception in all three analgesic tests. However, arecaidine, at the same i.c.v. doses, was able to reduce the pain threshold in the hot-plate and paw pressure tests.4. The site of muscarinic control of the pain threshold is localized in the CNS since drugs which do not cross the blood-brain barrier such as McN-A-343, pirenzepine and arecaidine exerted their effects only if injected i.c.v.5. On the basis of the above findings and existing literature we suggest that the postsynaptic muscarinic receptors involved in antinociception belong to the M1 subtype. Nevertheless, presynaptic autoreceptors (M2 subtype) may play a role in pain regulation since they are involved in modulation of endogenous ACh release.
Topics: (4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride; Analgesia; Animals; Male; Mice; Pain Measurement; Pirenzepine; Quinuclidines; Receptors, Muscarinic; Thiophenes
PubMed: 1375858
DOI: 10.1111/j.1476-5381.1992.tb14213.x -
American Journal of Obstetrics and... Dec 2014Presently, 97.7% of prescriptions for the treatment of nausea and vomiting in pregnancy in the United States are with medications not labeled for use in pregnancy, not...
Presently, 97.7% of prescriptions for the treatment of nausea and vomiting in pregnancy in the United States are with medications not labeled for use in pregnancy, not indicated for nausea and vomiting in pregnancy, and not classified as safe in pregnancy by the Food and Drug Administration. The use of ondansetron for nausea and vomiting in pregnancy has increased from 50,000 monthly prescriptions in 2008 to 110,000 at the end of 2013, despite unresolved issues regarding fetal safety and Food and Drug Administration warnings about serious dysrhythmias. In April 2013, the Food and Drug Administration approved the combination of doxylamine and pyridoxine, specifically for nausea and vomiting in pregnancy symptoms. Now that a safe and effective drug is available in the United States, there is no reason for women to be exposed to a drug of unproven maternal and fetal safety.
Topics: Antiemetics; Dicyclomine; Doxylamine; Drug Approval; Drug Combinations; Female; Heart Defects, Congenital; Humans; Morning Sickness; Ondansetron; Practice Patterns, Physicians'; Pregnancy; Pyridoxine; Serotonin Syndrome; Torsades de Pointes; United States; United States Food and Drug Administration
PubMed: 25151184
DOI: 10.1016/j.ajog.2014.08.017 -
Canadian Medical Association Journal Nov 1983
Topics: Abnormalities, Drug-Induced; Canada; Dicyclomine; Doxylamine; Drug Combinations; Drug Industry; Female; Humans; Infant, Newborn; Legislation, Drug; Male; Pregnancy; Public Opinion; Pyridines; Pyridoxine; United States
PubMed: 6627167
DOI: No ID Found -
Indian Journal of Pharmacology 2017The study was designed to evaluate possible antihistaminic and anticholinergic activities of . (Comparative Study)
Comparative Study
OBJECTIVE
The study was designed to evaluate possible antihistaminic and anticholinergic activities of .
MATERIALS AND METHODS
Effects of crude ethanolic (Ed.Eth) and effects of crude aqueous (Ed.Aq) extracts of were studied using isolated guinea pig ileum, rabbit jejunum, and rabbit trachea. Tissue responses were recorded using isotonic and isometric transducers, connected with PowerLab data acquisition system.
RESULTS
A dose-dependent (0.1-0.3 mg/ml) rightward shift was demonstrated in histamine concentration-response curves. Whereas a complete relaxation of carbachol (1 μM)-induced contractions in isolated rabbit jejunum (3 mg/ml) and tracheal (10 mg/ml) preparations was observed, similar to dicyclomine at 1 and 3 μM, respectively. However, no significant difference between the effects of Ed.Eth and Ed.Aq was observed.
CONCLUSION
Study provides pharmacological evidence for the presence of antihistaminic and anticholinergic activities in crude extracts of and also highlight its medicinal significance in the management of airway and gastrointestinal disorders.
Topics: Animals; Cholinergic Antagonists; Dicyclomine; Dose-Response Relationship, Drug; Equisetum; Female; Guinea Pigs; Histamine Antagonists; Ileum; Jejunum; Male; Plant Extracts; Rabbits; Trachea
PubMed: 28458431
DOI: 10.4103/0253-7613.201017 -
Biological & Pharmaceutical Bulletin Dec 2004Dicyclomine hydrochloride is an antispasmodic agent. The MIC of dicyclomine against standard strains of Gram positive and Gram negative bacteria were performed by NCCLS... (Comparative Study)
Comparative Study
Dicyclomine hydrochloride is an antispasmodic agent. The MIC of dicyclomine against standard strains of Gram positive and Gram negative bacteria were performed by NCCLS broth dilution technique. These drugs showed a rapid killing action on Gram positive bacteria, Staphylococcus aureus NCTC 6571, 8530 and several other reference strains. The killing effect against Gram negative bacteria, Shigella boydii 8 NCTC 254/66 and Salmonella typhimurium NCTC 74 showed that the drug was bacteriostatic with respect to these strains. High rate of killing was achieved for most strains of Gram positive bacteria within 2 h. When administered to Swiss strain of white mice at doses of 30 and 60 microg/g of mouse, the drug could significantly protect the animals challenged with 50 MLD of Salmonella typhimurium NCTC 74. According to chi2 test, the in vivo data were highly significant (p<0.001). Since dicyclomine showed a remarkable inhibitory action against several pathogenic bacteria, in the course of time, it may be developed as a potent antimicrobial agent for many bacterial infections.
Topics: Animals; Anti-Bacterial Agents; Dicyclomine; Gram-Negative Bacteria; Gram-Positive Bacteria; Male; Mice; Microbial Sensitivity Tests
PubMed: 15577222
DOI: 10.1248/bpb.27.2010 -
Canadian Medical Association Journal Feb 1981
Topics: Abnormalities, Drug-Induced; Antiemetics; Dicyclomine; Doxylamine; Drug Combinations; Female; Humans; Infant, Newborn; Maternal-Fetal Exchange; Pregnancy; Pyridines; Pyridoxine; Teratogens
PubMed: 7459786
DOI: No ID Found -
British Medical Journal (Clinical... Oct 1985
Clinical Trial
Topics: Age Factors; Colic; Crying; Cyclohexanecarboxylic Acids; Dicyclomine; Humans; Infant
PubMed: 3931770
DOI: 10.1136/bmj.291.6501.1014