Differential receptor dependencies: expression and significance of muscarinic M1 receptors in the biology of prostate cancer
This study shows that the type 1 acetylcholine muscarinic receptor (CHRM1) contributes toward the proliferation and growth of prostate cancer. We used growth and cytotoxic assays, the prostate cancer microarray database and CHRM downstream pathways’ homology of CHRM subtypes to uncover multiple signals leading to the growth of prostate cancer. Growth assays showed that pilocarpine stimulates the proliferation of prostate cancer. Moreover, it shows that carbachol exerts an additional agonistic action on nicotinic cholinergic receptor of prostate cancer cells that can be blocked by tubocurarine. With the use of selective C...
Source: Anti-Cancer Drugs - December 1, 2016 Category: Cancer & Oncology Tags: Preclinical Reports Source Type: research
Pain-relieving agents for infantile colic.
CONCLUSIONS: At the present time, evidence of the effectiveness of pain-relieving agents for the treatment of infantile colic is sparse and prone to bias. The few available studies included small sample sizes, and most had serious limitations. Benefits, when reported, were inconsistent.We found no evidence to support the use of simethicone as a pain-relieving agent for infantile colic.Available evidence shows that herbal agents, sugar, dicyclomine and cimetropium bromide cannot be recommended for infants with colic.Investigators must conduct RCTs using standardised measures that allow comparisons among pain-relieving agent...
Source: Cochrane Database of Systematic Reviews - September 15, 2016 Category: Journals (General) Authors: Biagioli E, Tarasco V, Lingua C, Moja L, Savino F Tags: Cochrane Database Syst Rev Source Type: research
The Prokinetic, Laxative, and Antidiarrheal Effects of Morus nigra: Possible Muscarinic, Ca2+ Channel Blocking, and Antimuscarinic Mechanisms
This study demonstrates gut modulatory properties of M. nigra. The prokinetic, laxative, and antidiarrheal activities of M. nigra were assessed in mice, while isolated rabbit jejunum and guinea‐pig ileum were used to explore insight into mechanism(s). At 30 and 70 mg/kg, the crude extract of M. nigra (Mn.Cr) exhibited atropine‐sensitive prokinetic and laxative effects, similar to carbachol (CCh). While at higher doses (100, 300, and 500 mg/kg), Mn.Cr offered protection against castor oil‐induced diarrhea. In rabbit jejunum, Mn.Cr and its chloroform fraction inhibited CCh‐induced contractions more potently...
Source: Phytotherapy Research - May 26, 2016 Category: Biochemistry Authors: Anam Akhlaq, Malik Hassan Mehmood, Abdul Rehman, Zohaib Ashraf, Sadia Syed, Samira Ahmed Bawany, Anwarul‐Hassan Gilani, Maimoona Ilyas, Bina Shaheen Siddiqui Tags: Research Article Source Type: research
Proactive management strategies for potential gastrointestinal adverse reactions with ceritinib in patients with advanced ALK-positive non-small-cell lung cancer
Eric S Schaefer,1 Christina Baik2 1Section of Medical Oncology, Highlands Oncology Group, Fayetteville, AR, 2Department of Medicine, Medical Oncology Division, University of Washington School of Medicine, Seattle, WA, USA Abstract: Anaplastic lymphoma kinase (ALK) gene fusions occur in 3%–7% of non-small-cell lung cancer (NSCLC) cases. Ceritinib, a once-daily, oral ALK inhibitor, has activity against crizotinib-resistant and crizotinib-naïve NSCLC, including brain metastases. Ceritinib (Zykadia™) was granted accelerated approval by the US Food and Drug Administration in 2014 for treating crizotinib-resist...
Source: Cancer Management and Research - March 24, 2016 Category: Cancer & Oncology Tags: Cancer Management and Research Source Type: research
Effects of the M1 muscarinic antagonist dicyclomine on emotional memory retrieval.
Extensive research has shown the involvement of the central cholinergic system in the acquisition and consolidation of tasks involving conditioned fear responses, such as those observed in contextual fear conditioning (CFC), tone fear conditioning (TFC) and inhibitory avoidance (IA). However, there are few data concerning the role of this system in the memory retrieval process. Therefore, the present study aimed to compare the effects of the administration of an M1 antagonist on retrieval during these tasks. For each behavioral procedure, groups of male Wistar rats were trained. Twenty-four hr later, they were treated with...
Source: Behavioral Neuroscience - November 30, 2015 Category: Neuroscience Authors: Soares, Juliana Carlota Kramer; Perfetto, Juliano Genaro; Antonio, Bruno Brito; Oliveira, Maria Gabriela Menezes Source Type: research
Novel Therapies in IBS-D Treatment
Opinion statement
Irritable bowel syndrome (IBS) is a common gastrointestinal disease characterized by abdominal pain and change in bowel habits. IBS diarrhea predominant (IBS-D), which is arguably the most common subset of IBS, is also associated with rectal urgency, increased frequency, abdominal bloating, and loose to watery stools. Current treatments for diarrhea include mu-opioid agonists (i.e., loperamide, lomotil) and bile acid sequestrants (i.e., cholestyramine) while treatments for abdominal pain include antispasmodics (i.e., hyoscyamine, dicyclomine) and tricyclic antidepressants (i.e., amitript...
Source: Current Treatment Options in Gastroenterology - October 2, 2015 Category: Gastroenterology Source Type: research
Infantile Colic: Recognition and Treatment.
Abstract
Infantile colic is a benign process in which an infant has paroxysms of inconsolable crying for more than three hours per day, more than three days per week, for longer than three weeks. It affects approximately 10% to 40% of infants worldwide and peaks at around six weeks of age, with symptoms resolving by three to six months of age. The incidence is equal between sexes, and there is no correlation with type of feeding (breast vs. bottle), gestational age, or socioeconomic status. The cause of infantile colic is not known; proposed causes include alterations in fecal microflora, intolerance to co...
Source: American Family Physician - October 1, 2015 Category: Primary Care Authors: Johnson JD, Cocker K, Chang E Tags: Am Fam Physician Source Type: research
The Charms of the CHRM Receptors: Apoptotic and Amoebicidal effects of Dicyclomine on Acanthamoeba castellanii.
Abstract
G-protein coupled receptors (GPCRs) are conserved amongst the eukaryotic cells are known to perform vital functions. Recently, anticholinergic drugs that target muscarinic cholinergic receptors have been found to kill pathogenic protists like Acanthamoeba, Balamuthia mandrillaris and Naegleria fowleri. Because of these effects, it was logical to expect a primeval cholinergic counterpart of this receptor on Acanthamoeba. Bioinformatics searches were made at data banks of Acanthamoeba genome and proteome. Immunostaining was done by using anti-human muscarinic M-1 antibody. Incubation assays were per...
Source: Antimicrobial Agents and Chemotherapy - August 10, 2015 Category: Microbiology Authors: Baig AM Tags: Antimicrob Agents Chemother Source Type: research
Pharmacological justification of use of Solena heterophylla Lour. in gastrointestinal, respiratory and vascular disorders
Conclusions:
The observed relaxant effect may be outcome of anti-muscarinic and Ca2+ channel blocking activities. The Sh.Cr (0.03-1.0 mg/ml) against phenyephrine (1 μM)- and K+(80 mM)-induced contractions in isolated rabbit aortic preparations exerted a relaxant effect, possibly through Ca2+ channel blocking activity. These findings provide a rationale for the folkloric uses of the plant in the management of ailments pertaining to gastrointestinal, respiratory and vascular system. (Source: Journal of Translational Medicine)
Source: Journal of Translational Medicine - April 30, 2015 Category: Research Authors: Khalid JanbazTashfeen AkhtarFatima SaqibImran ImranMuhammad Zia-Ul-HaqChaweeewan JansakulVincenzo De FeoMarius Moga Source Type: research
Potentially Inappropriate Anticholinergic Medication Use in Community-Dwelling Older Adults: A National Cross-Sectional Study
Conclusion
The study found that approximately one in ten older adults used potentially inappropriate anticholinergic medications. Several predisposing, enabling and need factors were associated with the use of potentially inappropriate anticholinergic medications. Concerted efforts are needed to optimize potentially inappropriate anticholinergic medication use in older adults. (Source: Drugs and Aging)
Source: Drugs and Aging - April 1, 2015 Category: Geriatrics Source Type: research
Development and validation of a liquid chromatographic method for estimation of dicyclomine hydrochloride, mefenamic acid and paracetamol in tablets
DA Shah, Jainika P Rana, Usmangani K Chhalotiya, SL Baldania, KK BhattIndian Journal of Pharmaceutical Sciences 2014 76(6):529-534Liquid chromatographic method was developed for simultaneous quantitative determination of dicyclomine hydrochloride, mefenamic acid and paracetamol in their combined dosage form. The separation was achieved using a C 18 column (250×4.6 mm id, 5 μm) using acetonitrile:20 mM potassium dihydrogen phosphate 70:30 (v/v) adjusted to pH 4 using orthophosphoric acid as mobile phase at a flow rate of 1 ml/min and detection at 220 nm. Separation was completed within 12 min. The re...
Source: Indian Journal of Pharmaceutical Sciences - December 17, 2014 Category: Drugs & Pharmacology Authors: DA ShahJainika P RanaUsmangani K ChhalotiyaSL BaldaniaKK Bhatt Source Type: research
Pharmacological Basis for Medicinal Use of Lens culinaris in Gastrointestinal and Respiratory Disorders
Crude extract of Lens culinaris (Lc.Cr), which tested positive for presence of anthraquinones, flavonoids, saponins, sterol, tannins, and terpenes exhibited protective effect against castor oil‐induced diarrhea in mice at 100–1000 mg/kg. In rabbit jejunum preparations, Lc.Cr caused relaxation of spontaneous contractions at 0.03–5.0 mg/mL. Lc.Cr inhibited carbachol (CCh, 1 μM) and K+ (80 mM)‐induced contractions in a pattern similar to dicyclomine, but different from verapamil and atropine. Lc.Cr shifted the Ca++ concentration‐response curves to the right, like dicyclomine and verapamil. Pretreatment of t...
Source: Phytotherapy Research - March 1, 2014 Category: Biochemistry Authors: Munasib Khan, Arif‐ullah Khan, Najeeb‐ur‐ Rehman, Anwarul‐Hassan Gilani Tags: Research Article Source Type: research
Homeopathy for treatment of irritable bowel syndrome.
CONCLUSIONS: A pooled analysis of two small studies suggests a possible benefit for clinical homeopathy, using the remedy asafoetida, over placebo for people with constipation-predominant IBS. These results should be interpreted with caution due to the low quality of reporting in these trials, high or unknown risk of bias, short-term follow-up, and sparse data. One small study found no statistically difference between individualised homeopathy and usual care (defined as high doses of dicyclomine hydrochloride, faecal bulking agents and diet sheets advising a high fibre diet). No conclusions can be drawn from this study due...
Source: Cochrane Database of Systematic Reviews - November 13, 2013 Category: Journals (General) Authors: Peckham EJ, Nelson EA, Greenhalgh J, Cooper K, Roberts ER, Agrawal A Tags: Cochrane Database Syst Rev Source Type: research
IL-6 attenuates trimethyltin-induced cognitive dysfunction via activation of JAK2/STAT3, M1 mAChR and ERK signaling network.
Abstract
We previously reported that interleukin (IL)-6 deficiency potentiates trimethyltin (TMT)-induced convulsive neurotoxicity. The purpose in this study was to investigate the molecular mechanism by which cytokines affect TMT-induced cognitive impairment. To accomplish this, we examined hippocampal changes in Janus kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) signaling in relation to cholinergic parameters after TMT treatment in mice genetically deficient in IL-6 (IL-6(-/-)), tumor necrosis factor-α (TNF-α(-/-)), or interferon-γ (IFN-γ(-/-)). The IL-6(-/-) mice were t...
Source: Cellular Signalling - May 24, 2013 Category: Cytology Authors: Kim BK, Tran HY, Shin EJ, Lee C, Chung YH, Jeong JH, Bach JH, Kim WK, Park DH, Saito K, Nabeshima T, Kim HC Tags: Cell Signal Source Type: research
Effects of muscarinic agents on chick choroids in intact eyes and eyecups: evidence for a muscarinic mechanism in choroidal thinning
ConclusionsMuscarinic agonists caused choroidal thinning in intact eyes and eyecups, supporting a role for acetylcholine in the choroidal response to hyperopic defocus or form deprivation. Only oxotremorine stimulated eye growth, which is inconsistent with a muscarinic receptor mechanism for antagonist‐induced eye growth inhibition. The dissociation between choroidal thinning and ocular growth stimulation for the other agonists in vivo suggest separate pathways for the two. (Source: Ophthalmic and Physiological Optics)
Source: Ophthalmic and Physiological Optics - May 12, 2013 Category: Opthalmology Authors: Debora L Nickla, Xiaoying Zhu, Josh Wallman Tags: Original Article Source Type: research
