Displaying publications 1 - 20 of 139 in total

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  1. Methyl (SR)-10-chloro-1,2,3,4,5,6-hexahydro-6-hydroxy-8-methoxy-1-methyl-1,9-phenanthroline-6-carboxylate
    Usman A, Razak IA, Chantrapromma S, Fun HK, Sarkar TK, Basak S, et al.
    Acta Crystallogr C, 2001 Sep;57(Pt 9):1116-7.
    PMID: 11588389
    In the title compound, C(16)H(19)ClN(2)O(4), the pyridine ring is nearly planar, the piperidine ring is non-planar and the cyclohexane ring adopts a screw-boat conformation. The carboxylate group makes a dihedral angle of 80.9 (2) degrees with the least-squares plane through the cyclohexane ring.
    Matched MeSH terms: Cholinergic Agonists/chemistry*
  2. [Chemical studies on the analgesic indole alkaloids from the traditional medicine (Mitragyna speciosa) used for opium substitute]
    Takayama H, Aimi N, Sakai S
    Yakugaku Zasshi, 2000 Oct;120(10):959-67.
    PMID: 11082707
    The leaves of a tropical plant, Mitragyna speciosa Korth. (Rubiaceae), have been traditionally used as a substitute for opium. By phytochemical studies on the constituents of the plant growing in Thailand as well as in Malaysia, several 9-methoxy-Corynanthe-type monoterpenoid indole alkaloids including new natural products were isolated. The structures of these new compounds were elucidated by the modern spectroscopic methods and/or chiral-total syntheses. The chiral total synthesis of (-)-mitragynine, a major component of this plant, was achieved. Potent opioid agonistic properties of mitragynine, which acts on mu- and delta-opioid subtype receptors, and of mitragynine pseudoindoxyl, whose analgesic activity is more potent than that of morphine, were clarified in in vitro experiments. The essential structural features in mitragynine for revealing the analgesic activity were elucidated by pharmacological evaluation of the natural and synthetic mitragynine derivatives.
    Matched MeSH terms: Receptors, Opioid/agonists
  3. Comparative bioavailability study of two salbutamol tablets in healthy adult volunteers
    Chik Z, Basu RC, Pendek R, Lee TC, Mohamed Z
    Int J Clin Pharmacol Ther, 2009 Jun;47(6):413-8.
    PMID: 19473604
    This study was carried out to compare the rate and extent of absorption of a generic salbutamol in oral dosage form (Brethmol, 4 mg) with the proprietary equivalent product (Ventolin, 4 mg), in healthy adult subjects, under fasting conditions. The study was a single dose, randomized, two way crossover study with a four-week washout period. It involved 22 healthy volunteers who received a single dose (4 mg) of the test and the reference products after an overnight fast of at least 10 hours. Blood samples were collected at pre-dose and a serial of 14 samples were collected from each of the subject from 1 h until 48 h post-dose. Plasma concentrations of salbutamol were analyzed using GCMS method. The mean AUC(0-yen) values were 91.26 and 96.45 h.ng/ml for reference and test product, respectively. The mean C(max) values were 12.26 and 12.38 ng/ml and the mean t(max) values were 2.80 and 2.33 hours for reference and test product, respectively. Analysis of variance showed that the 90% confidence intervals on the relative difference of the ratio for the AUC(0-yen) and the C(max) for the test and reference products were contained within the bioequivalence limit (80 - 125%) (C(max): 89.8 - 110.5% and AUC(0-yen): 91.6 - 121.5%). There was no statistically significant difference for the t(max) between the test and reference formulations (p = 0.30). The test formulation was found to be bioequivalent to the reference formulation with regard to AUC(0-yen) and C(max). There was no statistically significant difference in Brethmol and Ventolin t(max). In conclusion, Brethmol and Ventolin are bioequivalent in healthy subjects.
    Matched MeSH terms: Adrenergic beta-Agonists/administration & dosage; Adrenergic beta-Agonists/blood; Adrenergic beta-Agonists/pharmacokinetics*
  4. Current Status and Challenges in Rotigotine Delivery
    Md S, Karim S, Saker SR, Gie OA, Hooi LC, Yee PH, et al.
    Curr Pharm Des, 2020;26(19):2222-2232.
    PMID: 32175832 DOI: 10.2174/1381612826666200316154300
    Rotigotine is a non-ergoline, high lipophilic dopamine agonist. It is indicated as the first-line therapy for Parkinson's disease (PD) and Restless Leg Syndrome (RLS). However, the precise mechanism of rotigotine is yet to be known. Rotigotine has similar safety and tolerability to the other oral non-ergolinic dopamine antagonists in clinical trials, which include nausea, dizziness and somnolence. Neupro® was the first marketed transdermal patch formulation having rotigotine. The transdermal delivery system is advantageous as it enables continuous administration of the drug, thus providing steady-state plasma drug concentration for 24-hours. Intranasal administration of rotigotine allows the drug to bypass the blood-brain barrier enabling it to reach the central nervous system within minutes. Rotigotine can also be formulated as an extended-release microsphere for injection. Some challenges remain in other routes of rotigotine administration such as oral, parenteral and pulmonary, whereby resolving these challenges will be beneficial to patients as they are less invasive and comfortable in terms of administration. This review compiles recent work on rotigotine delivery, challenges and its future perspective.
    Matched MeSH terms: Dopamine Agonists
  5. A novel sponge-derived protein thrombocorticin is a new agonist for thrombopoietin receptor
    Watari H, Nakajima H, Atsuumi W, Nakamura T, Nanya T, Ise Y, et al.
    Comp Biochem Physiol C Toxicol Pharmacol, 2019 Jul;221:82-88.
    PMID: 30978513 DOI: 10.1016/j.cbpc.2019.04.003
    We screened 868 marine extracts in search of hematopoietic molecules resulted in findings of several extracts that proliferated Ba/F3-HuMpl cells but not the cells expressed with other hematopoietic cytokine receptors, EPO and G-CSF. Separation of the most potent extract of a Micronesian sponge Corticium sp., guided by the cell proliferation assay using Ba/F3-HuMpl cells resulted in an isolation of thrombocorticin (ThC), a novel 14 kDa protein as an active principal. ThC displayed concentration-dependent proliferation of Ba/F3-HuMpl cells, and had a stronger activity than that of eltrombopag, a small molecule drug used to treat thrombocytopenia. ThC induced phosphorylation of STAT5, suggesting that it activates Jak/STAT pathway as in the case of TPO. These results together indicated that ThC is a specific agonist for c-Mpl, although the size and shape differs largely from TPO. Here we present isolation, characterization and biological activity of ThC.
    Matched MeSH terms: Receptors, Thrombopoietin/agonists*
  6. Cardiorenal diseases in type 2 diabetes mellitus: clinical trials and real-world practice
    Lim LL, Chow E, Chan JCN
    Nat Rev Endocrinol, 2023 Mar;19(3):151-163.
    PMID: 36446898 DOI: 10.1038/s41574-022-00776-2
    Patients with type 2 diabetes mellitus (T2DM) can have multiple comorbidities and premature mortality due to atherosclerotic cardiovascular disease, hospitalization with heart failure and/or chronic kidney disease. Traditional drugs that lower glucose, such as metformin, or that treat high blood pressure and blood levels of lipids, such as renin-angiotensin-system inhibitors and statins, have organ-protective effects in patients with T2DM. Amongst patients with T2DM treated with these traditional drugs, randomized clinical trials have confirmed the additional cardiorenal benefits of sodium-glucose co-transporter 2 inhibitors (SGLT2i), glucagon-like peptide 1 receptor agonists (GLP1RA) and nonsteroidal mineralocorticoid receptor antagonists. The cardiorenal benefits of SGLT2i extended to patients with heart failure and/or chronic kidney disease without T2DM, whereas incretin-based therapy (such as GLP1RA) reduced cardiovascular events in patients with obesity and T2DM. However, considerable care gaps exist owing to insufficient detection, therapeutic inertia and poor adherence to these life-saving medications. In this Review, we discuss the complex interconnections of cardiorenal-metabolic diseases and strategies to implement evidence-based practice. Furthermore, we consider the need to conduct clinical trials combined with registers in specific patient segments to evaluate existing and emerging therapies to address unmet needs in T2DM.
    Matched MeSH terms: Glucagon-Like Peptide-1 Receptor/agonists
  7. Changing paradigms in the treatment of asthma
    Loh LC
    Family Physician, 2005;13:5-9.
    Significant changes have occurred in relation to how chronic asthma is being treated. Emphasis has now shifted from viewing asthma as a condition of smooth muscle dysfunction to one of chronic inflammation. As such, anti-inflammatory therapy forming the cornerstone of treatment represents the first important milestone in the evolution of asthma treatment. For this purpose, inhaled corticosteroid (ICS) is by far the most effective anti-inflammatory therapy. Another important milestone is the recognition of the superiority of adding long-acting beta2-agonist (LABA) to ICS over escalating ICS dose alone or other forms of add-on therapies in treating asthmatic patients not responding to regular ICS alone. The effectiveness of adding LABA to ICS in treating asthma logically led to combining the two drugs into one single inhaler (salmeterol/fluticasone and budesonide/formoterol) that has the attractiveness of being user-friendly and ensuring that ICS is not missed out. The unique property of formoterol that allows for repetitive flexible dosing paved way to the concept of using Symbicort for both regular maintenance dosing and as required rescue medication. This revolutionary approach has been recently shown to provide improved asthma outcome, achieved at an overall lower or at least comparable corticosteroid intake, and may represent another evolutionary step in the treatment strategy of chronic asthma. Keywords: Asthma treatment, airway inflammation, corticosteroid, long-acting beta2-agonist
    Matched MeSH terms: Adrenergic beta-Agonists
  8. The effect of multiple simulation parameters on MM/PBSA performance for binding affinity prediction of CB1 cannabinoid receptor agonists and antagonists
    Loo JSE, Yong AYY, Yong YN
    Chem Biol Drug Des, 2020 11;96(5):1244-1254.
    PMID: 32462752 DOI: 10.1111/cbdd.13733
    Both the inactive- and active-state CB1 receptor crystal structures have now been solved, allowing their application in various structure-based drug design methods. One potential method utilizing these crystal structures is the Molecular Mechanics/Poisson-Boltzmann Surface Area (MM/PBSA) method of predicting relative binding free.
    Matched MeSH terms: Cannabinoid Receptor Agonists/metabolism; Cannabinoid Receptor Agonists/pharmacology*
  9. In vitro functional evaluation of isolaureline, dicentrine and glaucine enantiomers at 5-HT2 and α1 receptors
    Heng HL, Chee CF, Thy CK, Tee JT, Chin SP, Herr DR, et al.
    Chem Biol Drug Des, 2019 02;93(2):132-138.
    PMID: 30216681 DOI: 10.1111/cbdd.13390
    Compounds with activity at serotonin (5-hydroxytryptamine) 5-HT2 and α1 adrenergic receptors have potential for the treatment of central nervous system disorders, drug addiction or overdose. Isolaureline, dicentrine and glaucine enantiomers were synthesized, and their in vitro functional activities at human 5-HT2 and adrenergic α1 receptor subtypes were evaluated. The enantiomers of isolaureline and dicentrine acted as antagonists at 5-HT2 and α1 receptors with (R)-isolaureline showing the greatest potency (pKb  = 8.14 at the 5-HT2C receptor). Both (R)- and (S)-glaucine also antagonized α1 receptors, but they behaved very differently to the other compounds at 5-HT2 receptors: (S)-glaucine acted as a partial agonist at all three 5-HT2 receptor subtypes, whereas (R)-glaucine appeared to act as a positive allosteric modulator at the 5-HT2A receptor.
    Matched MeSH terms: Adrenergic alpha-1 Receptor Agonists/metabolism; Adrenergic alpha-1 Receptor Agonists/chemistry; Serotonin 5-HT2 Receptor Agonists/metabolism; Serotonin 5-HT2 Receptor Agonists/chemistry
  10. Fulltext Acute pancreatitis as a rare adverse event among cannabis users: A systematic review
    Jaiswal V, Mukherjee D, Batra N, Ruchika F, Susheela AT, Chia JE, et al.
    Medicine (Baltimore), 2022 Jul 01;101(26):e29822.
    PMID: 35777067 DOI: 10.1097/MD.0000000000029822
    BACKGROUND: Cannabis use has been steadily rising in the United States and can have multiple adverse effects, including cannabis-induced acute pancreatitis. This study aims to collate and highlight the significant demographics, clinical presentation, and outcomes in patients with cannabis-induced acute pancreatitis.

    METHOD: A systematic literature search of electronic databases for peer-reviewed articles was conducted. After an initial search, we found 792 articles through different electronic databases. After manually removing duplicates and articles that did not meet the criteria, 25 articles were included in our review.

    RESULTS: A total of 45 patients were studied, 35 (78%) cases were male and 10 (22%) cases were female, showing male predominance. The mean age of all participants was 29.2 ± 10.3 years. The most common presenting symptoms were abdominal pain 21 of 21 (100%), nausea 17 of 21 (81%), and vomiting 12 of 20 (60%). Ultrasound was normal in the majority of patients, with findings of mild pancreatitis. Computerized tomography scans revealed pancreatic edema and inflammation in 7 of 20 (35%) patients, and findings of necrotizing pancreatitis and complex fluid collection were visualized in 3 of 20 (15%) patients. Dilatation of intrahepatic or extrahepatic biliary ducts was not seen in any patients. The overall prognosis was good, with reported full recovery.

    CONCLUSIONS: Cannabis should be included in the differential diagnosis for the etiology of acute pancreatitis, which would help in early intervention and treatment for the mitigation of the rapidly progressive disease.

    Matched MeSH terms: Cannabinoid Receptor Agonists
  11. The beer component hordenine inhibits alcohol addiction-associated behaviours in mice
    Li Y, Vogel C, Kalinichenko LS, Hübner H, Weikert D, Schaefer N, et al.
    Addict Biol, 2023 Aug;28(8):e13305.
    PMID: 37500485 DOI: 10.1111/adb.13305
    Alcohol consumption is a widespread behaviour that may eventually result in the development of alcohol use disorder (AUD). Alcohol, however, is rarely consumed in pure form but in fruit- or corn-derived preparations, like beer. These preparations add other compounds to the consumption, which may critically modify alcohol intake and AUD risk. We investigated the effects of hordenine, a barley-derived beer compound on alcohol use-related behaviours. We found that the dopamine D2 receptor agonist hordenine (50 mg/kg) limited ongoing alcohol consumption and prophylactically diminished relapse drinking after withdrawal in mice. Although not having reinforcing effects on its own, hordenine blocked the establishment of alcohol-induced conditioned place preference (CPP). However, it independently enhanced alcohol CPP retrieval. Hordenine had a dose-dependent inhibitory effect on locomotor activity. Chronic hordenine exposure enhanced monoamine tissue levels in many brain regions. Further characterization revealed monoaminergic binding sites of hordenine and found a strong binding on the serotonin and dopamine transporters, and dopamine D3 , and adrenergic α1A and α2A receptor activation but no effects on GABAA receptor or glycinergic signalling. These findings suggest that natural ingredients of beer, like hordenine, may work as an inhibitory and use-regulating factor by their modulation of monoaminergic signalling in the brain.
    Matched MeSH terms: Dopamine Agonists
  12. Beta amino acid-modified and fluorescently labelled kisspeptin analogues with potent KISS1R activity
    Camerino MA, Liu M, Moriya S, Kitahashi T, Mahgoub A, Mountford SJ, et al.
    J. Pept. Sci., 2016 Jun;22(6):406-14.
    PMID: 27282137 DOI: 10.1002/psc.2883
    Kisspeptin analogues with improved metabolic stability may represent important ligands in the study of the kisspeptin/KISS1R system and have therapeutic potential. In this paper we assess the activity of known and novel kisspeptin analogues utilising a dual luciferase reporter assay in KISS1R-transfected HEK293T cells. In general terms the results reflect the outcomes of other assay formats and a number of potent agonists were identified among the analogues, including β(2) -hTyr-modified and fluorescently labelled forms. We also showed, by assaying kisspeptin in the presence of protease inhibitors, that proteolysis of kisspeptin activity within the reporter assay itself may diminish the agonist outputs. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd.
    Matched MeSH terms: Kisspeptins/agonists*
  13. Brexpiprazole for the treatment of schizophrenia
    Yee A
    Expert Rev Neurother, 2016;16(2):109-22.
    PMID: 26650624 DOI: 10.1586/14737175.2016.1129901
    Brexpiprazole (OPC-34712) is a novel serotonin-dopamine activity modulator, which has recently been approved by the U.S Food and Drug Administration for the treatment of schizophrenia. The aim of this paper is to systematically synthesize all data of the efficacy, safety and tolerability of Brexpiprazole in treating schizophrenia. The terms 'Brexpiprazole', 'OPC-34712' and 'schizophrenia' were searched. A total of 12 clinical trials with 7 available data records were found. The pooled effect size of Brexpiprazole 1 mg, 2 mg and 4 mg were all superior to placebo in terms of the change from baseline in positive and negative syndrome scale (PANSS) total score at week 6 (weighted mean difference = -3.74, p = 0.044; weighted mean difference = -5.76, p 
    Matched MeSH terms: Dopamine Agonists/therapeutic use*
  14. A step ahead of PPARγ full agonists to PPARγ partial agonists: therapeutic perspectives in the management of diabetic insulin resistance
    Chigurupati S, Dhanaraj SA, Balakumar P
    Eur J Pharmacol, 2015 May 15;755:50-7.
    PMID: 25748601 DOI: 10.1016/j.ejphar.2015.02.043
    Described since long as a member of the nuclear receptor superfamily, peroxisome proliferator-activated receptors (PPARs) regulate the gene expression of proteins involved in glucose and lipid metabolism. PPARs indeed regulate several physiologic processes, including lipid homeostasis, adipogenesis, inflammation, and wound healing. PPARs bind natural or synthetic PPAR ligands can function as cellular sensors to regulate the gene transcription. Dyslipidemia, and type 2 diabetes mellitus (T2DM) with insulin resistance are treated using agonists of PPARα and PPARγ, respectively. The PPARγ is a key regulator of insulin sensitization and glucose metabolism, and therefore is considered as an imperative pharmacological target to combat diabetic metabolic disease and insulin resistance. Of note, currently available PPARγ full agonists like rosiglitazone display serious adverse effects such as fluid retention/oedema, weight gain, and increased incidence of cardiovascular events. On the other hand, PPARγ partial agonists are being suggested to devoid or having less incidence of these undesirable events, and are under developmental stages. Current research is on the way for the development of novel PPARγ partial agonists with enhanced therapeutic efficacy and reduced adverse effects. This review sheds lights on the current status of development of PPARγ partial agonists, for the management of T2DM, having comparatively less or no adverse effects to that of PPARγ full agonists.
    Matched MeSH terms: PPAR gamma/agonists*
  15. Fulltext Flavonoids with M1 muscarinic acetylcholine receptor binding activity
    Swaminathan M, Chee CF, Chin SP, Buckle MJ, Rahman NA, Doughty SW, et al.
    Molecules, 2014 Jun 27;19(7):8933-48.
    PMID: 24979399 DOI: 10.3390/molecules19078933
    Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer's disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at human cloned M1 muscarinic receptors. Several compounds were found to possess competitive binding affinity (Ki=40-110 µM), comparable to that of acetylcholine (Ki=59 µM). Despite the fact that these compounds lack a positively-charged ammonium group under physiological conditions, molecular modelling studies suggested that they bind to the orthosteric site of the receptor, mainly through non-polar interactions.
    Matched MeSH terms: Muscarinic Agonists/chemistry*
  16. Fulltext Can initial perceptions about quitting predict smoking cessation among Malaysian smokers?
    Yasin SM, Masilamani R, Ming MF, Koh D, Zaki RA
    Southeast Asian J. Trop. Med. Public Health, 2012 Mar;43(2):501-9.
    PMID: 23082600
    Perceived risks and benefits of quitting smoking may be important factors in successful treatment. This study examined the association between initial perceived risks and benefits of quitting smoking and outcomes during a two month smoking cessation attempt. Participants (n = 185) were treatment-seeking smokers attending two smoking cessation clinics in Klang Valley, Malaysia. They received structured behavioral therapy and free Nicotine Replacement Therapy (NRT). Prior to treatment, a 12 item Perceived Risks and Benefits Questionnaire (PRBQ) was administered. This was used to assess the smoker's initial perceptions during their quit attempt. Participants were re-contacted at the end of two months to determine their smoking status. The results show participants intending to quit demonstrated a greater understanding of the benefits of quitting smoking than the risks of quitting. Those with a higher education level had a greater understanding of the benefits of quitting (p = 0.02). PRBQ items, such as perceived risks of quitting (ie weight gain, negative affect, social ostracism, loss of enjoyment and craving) were not associated with abstinence at two months. However, those who perceived a benefit of higher physical attraction post-cessation were less likely to have stopped smoking at two months (OR 0.18; 95% CI 0.08-0.45). Other perceived benefits at baseline, such as health, general well-being, self-esteem, finances and social approval, were not associated with smoking cessation at two months. The results suggest that in our study population, smokers' baseline perceptions of the benefits of cessation of smoking prior to therapy are not associated with quit results at two months. Counseling patients regarding the advantages and disadvantages of quitting may have changed their perceptions during quitting process and should be further explored in future studies.
    Study site: Smoking cessation clinics, University Malaya and Universiti Teknology Mara, Klang Valley, Malaysia
    Matched MeSH terms: Nicotinic Agonists/administration & dosage
  17. Stability-indicating micellar electrokinetic chromatography method for the analysis of sumatriptan succinate in pharmaceutical formulations
    Al Azzam KM, Saad B, Tat CY, Mat I, Aboul-Enein HY
    J Pharm Biomed Anal, 2011 Dec 15;56(5):937-43.
    PMID: 21873014 DOI: 10.1016/j.jpba.2011.08.007
    A micellar electrokinetic chromatography method for the determination of sumatriptan succinate in pharmaceutical formulations was developed. The effects of several factors such as pH, surfactant and buffer concentration, applied voltage, capillary temperature, and injection time were investigated. Separation took about 5 min using phenobarbital as internal standard. The separation was carried out in reversed polarity mode at 20 °C, 26 kV and using hydrodynamic injection for 10s. Separation was achieved using a bare fused-silica capillary 50 μm×40 cm and background electrolyte of 25 mM sodium dihydrogen phosphate-adjusted with concentrated phosphoric acid to pH 2.2, containing 125 mM sodium dodecyl sulfate and detection was at 226 nm. The method was validated with respect to linearity, limits of detection and quantification, accuracy, precision and selectivity. The calibration curve was linear over the range of 100-2000 μg mL(-1). The relative standard deviations of intra-day and inter-day precision for migration time, peak area, corrected peak area, ratio of corrected peak area and ratio of peak area were less than 0.68, 3.48, 3.28, 2.97 and 2.83% and 2.01, 5.50, 4.46, 4.92 and 4.07%, respectively. The proposed method was successfully applied to the determinations of the analyte in tablet. Forced degradation studies were conducted by introducing a sample of sumatriptan succinate standard solution to different forced degradation conditions using neutral (water), basic (0.1 M NaOH), acidic (0.1 M HCl), oxidative (10% H(2)O(2)) and photolytic (exposure to UV light at 254 nm for 2 h). It is concluded that the stability-indicating method for sumatriptan succinate can be used for the analysis of the drug in various samples.
    Matched MeSH terms: Serotonin 5-HT1 Receptor Agonists/analysis*
  18. Fulltext Predictors of smoking cessation among staff in public Universities in Klang Valley, Malaysia
    Yasin SM, Masilamani R, Ming MF, Koh D
    Asian Pac J Cancer Prev, 2011;12(3):811-6.
    PMID: 21627389
    Smoking cessation studies are often performed in clinic based settings. The present example aimed to find predictors of success among staff in worksite smoking cessation programmes in two major public universities in Klang Valley, Malaysia. All staff from both universities received an open invitation via staff e-mail and letters to participate. At the start of treatment, participants were administered the Rhode Island Stress and Coping Questionnaire and Family Support Redding's Questionnaire. Behaviour therapy with free nicotine replacement therapy (NRT) were given as treatment. After two months, they were contacted to determine their smoking status. 185 staff from University A (n=138) and University B (n=47), responded and voluntarily showed interest to quit. There was no significant difference in respondents with respect to socio demographic characteristics and smoking history. After two months of treatment, quit rates were 24% in University A vs. 38 % in University B (p>0.05). Univariate predictors of cessation were adherence to NRT (p<0.001), smoking fewer cigarettes per day (p<0.05) and the number of behaviour therapy sessions attended (p<0.001). Logistic regression identified 3 significant predictors of smoking cessation. Participants attending more than one session (OR= 27.00; 95% CI : 6.50; 111.6), and having higher pre-treatment general stress (OR= 2.15; 95% CI: 1.14; 4.05) were more likely to quit, while a higher number of cigarettes smoked (OR= 0.19: 95% CI: 0.06; 0.59) reduced the likelihood of quitting. Increasing age, ability to cope with stress and family support were not significant predictors. We conclude that factors such as the number of counseling sessions, the amount of cigarettes smoked at baseline, adherence to NRT and pretreatment stress are important considerations for success in a worksite smoking cessation programme.
    Matched MeSH terms: Nicotinic Agonists/administration & dosage*
  19. Discovery of new nanomolar peroxisome proliferator-activated receptor γ activators via elaborate ligand-based modeling
    Al-Najjar BO, Wahab HA, Tengku Muhammad TS, Shu-Chien AC, Ahmad Noruddin NA, Taha MO
    Eur J Med Chem, 2011 Jun;46(6):2513-29.
    PMID: 21482446 DOI: 10.1016/j.ejmech.2011.03.040
    Peroxisome Proliferator-Activated Receptor γ (PPARγ) activators have drawn great recent attention in the clinical management of type 2 diabetes mellitus, prompting several attempts to discover and optimize new PPARγ activators. With this in mind, we explored the pharmacophoric space of PPARγ using seven diverse sets of activators. Subsequently, genetic algorithm and multiple linear regression analysis were employed to select an optimal combination of pharmacophoric models and 2D physicochemical descriptors capable of accessing self-consistent and predictive quantitative structure-activity relationship (QSAR) (r2(71)=0.80, F=270.3, r2LOO=0.73, r2PRESS against 17 external test inhibitors=0.67). Three orthogonal pharmacophores emerged in the QSAR equation and were validated by receiver operating characteristic (ROC) curves analysis. The models were then used to screen the national cancer institute (NCI) list of compounds. The highest-ranking hits were tested in vitro. The most potent hits illustrated EC50 values of 15 and 224 nM.
    Matched MeSH terms: PPAR gamma/agonists*
  20. Ramelteon: a melatonin receptor agonist for the treatment of insomnia
    Devi V, Shankar PK
    J Postgrad Med, 2008 2 26;54(1):45-8.
    PMID: 18296808
    Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for the treatment of insomnia characterized by difficulty in sleep onset. It is a nonscheduled drug since it lacks the potential for abuse and does not interact with neurotransmitter receptors most associated with these phenomena. Although the effects of ramelteon use > 5 weeks are unknown, the available data confirms its safety and efficacy for short-term use. Clinical use and future research should uncover more information about ramelteon's properties.
    Matched MeSH terms: Receptors, Melatonin/agonists*
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