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1.
Reumatologia ; 62(2): 83-93, 2024.
Article in English | MEDLINE | ID: mdl-38799780

ABSTRACT

Introduction: The aims were to study the sociodemographic characteristics of patients presenting to the clinic and to study the clinical and serological pattern of systemic lupus erythematosus (SLE) in a new rheumatology clinic of a predominantly Yoruba population. Material and methods: This was a retrospective, cross-sectional study conducted over 7 years (January 2017 - December 2023). Patients who satisfied the 1997 American College of Rheumatology (ACR) and/or the 2012 Systemic Lupus International Collaborating Clinics (SLICC) classification criteria were enrolled using their medical records. Patients with overlap syndromes and other inflammatory or noninflammatory rheumatic diseases were excluded from the study. Their sociodemographic, clinical, laboratory, and treatment data were retrieved from their medical records and analysed using IBM SPSS version 23.0 software. Results: A total of 65 patients were diagnosed with SLE with a frequency of 15.8%. The mean age ±SD of the patients at presentation was 33.85 years ±11.01 and the female to male ratio was 9.8 : 1. The median (IQR) duration of symptoms at presentation was 7.0 months (3-24). The common clinical presentations included synovitis (86.2%), acute cutaneous rash (53.8%), oral ulcers (52.3%), nonscarring alopecia (50.8%), and serositis (47.7%). Proteinuria was seen in 37.7% of the patients and the predominant renal histopathological feature was Class IV. Antinuclear antibody was 100% positive with 50.94% of the patients having a titre of 1 : 5,120 and above. Anti-double-stranded deoxyribonucleic acid and anti-Smith antibodies each had 50% prevalence. Dyslipidaemia was found in 76.7% of the patients. Conclusions: The study's findings are largely consistent with similar studies done in Africa. Further prospective multi-centred studies are needed to further determine the epidemiological characteristics of the disease in Nigeria with a multi-ethnic population.

2.
Niger Postgrad Med J ; 31(1): 53-61, 2024 Jan 01.
Article in English | MEDLINE | ID: mdl-38321797

ABSTRACT

BACKGROUND: Improvements in sickle cell disease (SCD) care have resulted in the survival of many patients into adulthood, although this is accompanied by the increased incidence of end-organ damage, including chronic kidney disease (CKD). OBJECTIVES: This study assessed the prevalence, pattern and predictors of renal dysfunction in SCD patients and investigated the associated renal histopathologic changes. METHODS: We evaluated 105 patients with SCD, for proteinuria, estimated glomerular filtration rate (eGFR), and tubular dysfunction. Renal biopsy was conducted on 22 patients who qualified. Data were analysed using SPSS package version 23. RESULTS: Thirty-seven (35.2%) of the 105 patients had CKD, as defined by an eGFR of 60 ml/min/1.73 m2 and/or proteinuria. The fractional excretion of potassium (FEK) was elevated in all patients, whereas the fractional excretion of sodium (FENa) was elevated in 98.1%. Glomerular filtration rate was negatively correlated with irreversible percentage sickle cell count (r = -0.616, P = 0.0001), FEK (r = -0.448, P = 0.0001) and FENa (r = -0.336, P = 0.004). Age, irreversible percentage sickle cell count, haemoglobin levels and FENa were the major predictors of CKD. The histological pattern in the 22 patients who had biopsies was consistent with mesangioproliferative glomerulonephritis 11 (50%), minimal change disease 6 (27.3%), focal segmental glomerulosclerosis 3 (13.6%) and interstitial nephritis 2 (9.1%). CONCLUSIONS: CKD was prevalent in SCD patients, and it was characterised by tubular dysfunction and mesangioproliferative glomerulonephritis. The main predictors of CKD were increased age, severity of vaso-occlusive crisis, worsening anaemia and tubular dysfunction.


Subject(s)
Anemia, Sickle Cell , Glomerulonephritis , Renal Insufficiency, Chronic , Humans , Nigeria , Anemia, Sickle Cell/complications , Renal Insufficiency, Chronic/complications , Proteinuria/complications , Glomerular Filtration Rate , Glomerulonephritis/complications
3.
Eur Heart J Suppl ; 23(Suppl B): B114-B116, 2021 May.
Article in English | MEDLINE | ID: mdl-34248435

ABSTRACT

The aim of this study is to estimate the frequency of undetected hypertension across the six geopolitical zones of Nigeria. We conducted an opportunistic screening of adults aged at least 18 years in the month of May 2019. Participants were recruited by trained volunteers using the May Measurement Month protocol. Blood pressure (BP) was measured using validated digital and mercury sphygmomanometers. We defined hypertension as BP ≥140/90 mmHg or the use of BP-lowering medication. A total of 3646 participants (52.8% females) with a mean age of 44.5 ± 15.7 years were screened. Hypertension was present in 39.2% of the participants but only 55. 4% of these were on antihypertensive medications. Only 46.8% hypertensives who were on medications had their BP controlled (<140/90 mmHg). Previous history of hypertension in pregnancy, alcohol intake and smoking were associated with increased mean systolic and diastolic BPs. The frequency of Nigerians with hypertension is high while only about half of those on antihypertensive medications are controlled. A multi-pronged approach to reduce the burden of hypertension is needed.

4.
Clin Med Insights Cardiol ; 13: 1179546819852941, 2019.
Article in English | MEDLINE | ID: mdl-31258338

ABSTRACT

BACKGROUND: Cardiovascular disease (CVD) is the leading cause of mortality in patients with chronic kidney disease (CKD). Carotid intima-media thickness (CIMT) is a measure of atherosclerotic vascular disease and considered a comprehensive picture of all alterations caused by multiple cardiovascular risk factors over time on the arterial walls. We therefore sought to determine the CIMT of the common carotid artery in patients with CKD and to evaluate the clinical pattern and prevalence of CVD in CKD patients. METHODS: A case-control study involving 100 subjects made of 50 patients with CKD stages 2 to 4 and 50 age and sex matched apparently normal individuals. Carotid intima-media thickness of the common carotid artery was considered thickened if it measured greater than 0.8 mm. All subjects had laboratory investigations, 12-lead electrocardiogram, transthoracic echocardiography, and ankle-brachial index. RESULTS: The mean CIMT was higher in CKD population compared with controls (P < .001). Eighty-four percent of the study population was found to have thickened CIMT compared with 18% of controls (P < .001). Patients with CKD had significantly higher blood pressure and heart rate than controls. Cardiovascular disease was also more prevalent among patients with CKD as compared with controls. Carotid intima-media thickness positively correlated with age, blood pressure, and random blood sugar. CONCLUSIONS: As CIMT was well correlated with many cardiovascular risk factors among CKD patients, it may serve as a surrogate marker for CVD and its early assessment may target patients who may need more aggressive therapy to retard the progression of kidney disease and improve outcome.

5.
Afr Health Sci ; 19(4): 2863-2873, 2019 Dec.
Article in English | MEDLINE | ID: mdl-32127862

ABSTRACT

INTRODUCTION: Hypertension is a cause and consequence of chronic kidney disease globally. The other factors that work in concert with hypertension to cause CKD are yet to be clearly elucidated. Studies have identified proteinuria, dyslipidemia, obesity, smoking and family history of CKD as renal risk factors. Due to the high morbidity and mortality associated with occurrence of CKD including the enormous financial burden involved in its management, the knowledge of prevention and understanding of the risk factors for development of CKD is highly essential. Therefore, Identifying well defined risk factors that display strong graded association with the occurrence and progression of CKD can help in elucidating potential targets for disease modification. OBJECTIVE: The aim of this study was to determine the prevalence of renal risk factors and their impact on kidney function in newly diagnosed hypertensive Nigerians. METHODS: This was a case control study of two hundred and fifty newly diagnosed hypertensive Nigerians recruited from two contiguous hospitals in an urban setting in south western Nigeria. Another group of two hundred and fifty apparently healthy age and sex matched normotensive Nigerians in the same community were recruited as controls. RESULTS: Seventy (28%) of the newly diagnosed hypertensives had estimated glomerular filtration rate of less than 60ml/min, while 42.4% and 18.8% of the subjects and the controls had microalbuminuria respectively. The newly diagnosed hypertensives had significantly higher prevalence of analgesic use (86.4% versus 41.6%, p < 0.001), alcohol consumption (20.8% versus 12%, p = 0.008), use of canned salted food (18.8% versus 8.4%, p= 0.001) and central obesity (36.1% versus 26.8%, p= 0.025) compared to controls. CONCLUSION: There is a significant occurrence of modifiable renal risk factors in newly diagnosed hypertensives and this offers a platform for instituting preventive strategies in the community.


Subject(s)
Hypertension/epidemiology , Renal Insufficiency, Chronic/epidemiology , Urban Population/statistics & numerical data , Adult , Aged , Case-Control Studies , Comorbidity , Female , Glomerular Filtration Rate , Humans , Hypertension/diagnosis , Male , Middle Aged , Nigeria/epidemiology , Prevalence , Renal Insufficiency, Chronic/diagnosis , Risk Factors
6.
Afr Health Sci ; 18(3): 671-680, 2018 Sep.
Article in English | MEDLINE | ID: mdl-30603000

ABSTRACT

INTRODUCTION: Autosomal Dominant Polycystic Kidney Disease (ADPKD) is presumably rare in Africa. Knowledge about the disease in Nigeria is limited as demonstrated by scanty articles on the subject. OBJECTIVES: To determine the pattern of clinical presentation and outcome of ADPKD among ADPKD patients. METHOD: ADPKD subjects were prospectively studied between January 1996 and December 2010. Their demographics, clinical and investigation parameters were documented. Dependency on dialysis, renal transplant and death were the final outcomes. RESULTS: Forty one patients (M:F=1.3:1) with mean age of 48.6±4.6 years were studied. ADPKD was diagnosed at 2.73 cases per annum. Family history of ADPKD and hypertension were present in 56.1% and 82.9% respectively. Their mean systolic and diastolic blood pressures were 166.9 ±23.6 and 104 ±21.2 respectively.Nocturia (78.0%) and loin pain (68.3%) were the most common presenting symptoms. Liver cysts (31.7%) and aortic regurgitation (22.0%) were the predominant extra-renal manifestations.Twenty three (56.1%) received haemodialysis; no renal transplantation. Death rate was 51.2%. Presence of uraemia and intra-cerebral aneurysm contributed significantly to mortality. CONCLUSION: ADPKD may not be so rare in Nigeria. Awareness campaign to change attitude of family members to screening and further studies using newer criteria for diagnosis of ADPKD should be conducted.


Subject(s)
Polycystic Kidney, Autosomal Dominant/pathology , Adolescent , Adult , Age of Onset , Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Nigeria/epidemiology , Polycystic Kidney, Autosomal Dominant/epidemiology , Polycystic Kidney, Autosomal Dominant/mortality , Polycystic Kidney, Autosomal Dominant/therapy , Renal Dialysis , Young Adult
7.
Clin Nephrol ; 86 (2016)(13): 53-60, 2016.
Article in English | MEDLINE | ID: mdl-27509585

ABSTRACT

Kidney diseases have assumed epidemic proportions in both developed and developing countries, particularly chronic kidney disease (CKD). While treatment modalities are available and accessible in developed economies with improvement in outcomes, survival, and quality of life, they are either unavailable or inaccessible in nations with emerging economies, particularly in sub-Saharan Africa (SSA), with an attendant worsening outcome and survival for CKD patients. The epidemiology of CKD in SSA has revealed that it preferentially affects adults in their economically productive years, usually below the age of 50 years, with consequent drain on the economy. This derives mainly from the major etiologies in the region, which are infection-induced chronic glomerulonephritis and hypertension, compounded by poverty as well as societal and health underdevelopment, poor resource allocation to health, and underdeveloped health infrastructures. This has made preventive nephrology a major goal in the sub-region, although those who have already developed CKD must be managed up to tertiary levels. In this review, we assessed the contributions of parasitic diseases (i.e., malaria and schistosomiasis), sickle cell disease and nephrotoxins with the aim of espousing their contributions to the burden of kidney disease, and proposing management options with the goal of ultimately reducing the burden of kidney disease in these disadvantaged populations.


Subject(s)
Anemia, Sickle Cell/complications , Malaria/complications , Renal Insufficiency, Chronic/etiology , Schistosomiasis/complications , Africa South of the Sahara , Age Factors , Cost of Illness , Developing Countries , Glomerulonephritis/complications , Humans , Hypertension/complications , Renal Insufficiency, Chronic/parasitology , Survival Rate , Vulnerable Populations
8.
Int J Nephrol Renovasc Dis ; 7: 347-52, 2014.
Article in English | MEDLINE | ID: mdl-25258555

ABSTRACT

BACKGROUND: Nephrologists are faced with enormous challenges in the management of patients with end-stage renal disease, especially in sub-Saharan Africa, where hemodialysis is the most common modality of renal replacement therapy in the region. Therefore, we reviewed our 3 years of experience with hemodialysis services in a tertiary hospital located in a rural community of South West Nigeria. This was with a view to presenting the profile of hemodialysis patients and the challenges they face in sustaining hemodialysis. METHODS: We reviewed the case records and hemodialysis registers for 176 patients over the 3 years from November 2010 to December 2013. The data were analyzed using Statistical Package for the Social Sciences version 20 software. RESULTS: Of the 176 patients, 119 (66.9%) were males. The mean age of the patients was 44.87±17.21 years. Most were semiskilled or unskilled (111; 63.5%) and 29 (16.5%) were students. Twenty-six (14.8%) had acute kidney injury in the failure stage. Chronic glomerulonephritis, hypertensive nephropathy, and diabetic nephropathy accounted for 45.3%, 23.3%, and 12.1%, respectively, of patients with end-stage renal disease. Only 6.8% of patients could afford hemodialysis beyond 3 months. CONCLUSION: Sustainability of maintenance hemodialysis is poor in our environment. Efforts should be intensified to improve other modalities of renal replacement therapy, in particular kidney transplantation, which is cost-effective in the long-term. Also, preventive measures such as education for affected patients and the general population would assist in reducing the prevalence and progression to end-stage renal disease.

9.
Int J Gen Med ; 6: 19-24, 2013.
Article in English | MEDLINE | ID: mdl-23345988

ABSTRACT

PURPOSE: To determine whether low dose aspirin has any deleterious effects on renal function in elderly patients. METHODS: We conducted a prospective pilot study of 30 Nigerians older than 60 years with various chronic ailments necessitating the use of low dose aspirin. Patients gave their consent, and institutional ethical clearance was obtained. Each patient's baseline samples at enrolment (before commencing aspirin use) served as a control, and subsequent weekly samples were compared. The weekly mean of each parameter was calculated, and the differences of means from baseline were determined, and values were compared for statistical differences with the Statistical Package for the Social Sciences, version 16. RESULTS: We found that a majority of patients (86.67%) had basal renal functions at chronic kidney disease stages 1 and 2. When compared with the corresponding baseline parameters, the mean weekly serum and urinary electrolytes, urea, creatinine, and uric acid parameters did not change, and the P-value did not show any statistical significance. However, there was positive statistical significance for the creatinine clearance (P = 0.025). Also, unlike in previous studies, anemia and hypoalbuminemia did not affect the renal function parameters. CONCLUSION: This study did not show any deleterious effects with short-term, low dose (75 mg daily) aspirin use on kidney functions in elderly patients. However, caution should be exercised when dealing with patients in renal stages 3-5 and the very elderly, aged ≥ 80 years.

10.
Saudi J Kidney Dis Transpl ; 23(6): 1315-9, 2012 Nov.
Article in English | MEDLINE | ID: mdl-23168876

ABSTRACT

The morbidity and mortality from acute kidney injury (AKI) have remained relatively high over the last six decades. The triad of infections, nephrotoxins and obstetric complications are still major causes of acute kidney injury in the tropics. This retrospective study is a five-year audit of acute renal failure (ARF) (or stage 3 AKI) in patients requiring hemodialysis at the renal unit of the Department of Medicine of the Ladoke Akintola University of Technology (LAUTECH) Teaching Hospital, Osogbo, Nigeria. A total of 80 patients with AKI were treated over a five-year period at our center, of which 45 (56.2%) were in ARF, i.e. stage 3 AKI requiring hemodialysis. There were 24 males and 21 females. The most common cause of ARF among the patients was sepsis syndrome 16 (35.5%), while pregnancy-related cases accounted for 15 (33.3%) and nephrotoxins for 6 (13.3%). Five (33%) of the 15 pregnancy-related patients survived, and all were cases of septic abortion. Of the other 10 patients that did not survive, three (30%) had post-partum hemorrhage and seven (70%) post-partum eclampsia. In all, the mortality rate among our AKI presenting for hemodialysis at our center over a given year period was 28.8%. Majority of these were eclampsia related. The causes of ARF still remain the same in the tropics, eclampsia portends poor prognosis. Concerted efforts should be made at limiting this trend by active preventive services and early recognition of high-risk obstetrics cases.


Subject(s)
Acute Kidney Injury/therapy , Pregnancy Complications/therapy , Renal Dialysis , Tropical Climate , Abortion, Septic/etiology , Acute Kidney Injury/etiology , Acute Kidney Injury/mortality , Adolescent , Adult , Aged , Eclampsia/etiology , Female , Hospitals, University , Humans , Male , Middle Aged , Nigeria/epidemiology , Postpartum Hemorrhage/etiology , Pregnancy , Pregnancy Complications/etiology , Pregnancy Complications/mortality , Renal Dialysis/adverse effects , Renal Dialysis/mortality , Retrospective Studies , Risk Assessment , Risk Factors , Systemic Inflammatory Response Syndrome/complications , Time Factors , Treatment Outcome , Young Adult
11.
Article in English | MEDLINE | ID: mdl-23133316

ABSTRACT

An atrial septal aneurysm (ASA) is a rare but well-recognized abnormality of uncertain clinical relevance. It is a localized bulging of the inter-atrial septum into either or both atria during the cardiac cycle. ASA has been reported as an unexpected finding during autopsy but may also be diagnosed in living patients by echocardiographic techniques.We present a 37-year-old woman with a recurrent atypical chest pain of one-year duration. She was found to have a congenital atrial septal aneurysm on evaluation. The echocardiographic images mimicked a left sided cor triatriatum sinister. She had no other symptoms and had no co-morbidities. There was no audible murmur.ASA can mimic cor-triatriatum and echocardiographic examination should be performed from multiple views before any echocardiographic diagnosis is made.

12.
Pan Afr Med J ; 11: 75, 2012.
Article in English | MEDLINE | ID: mdl-22655109

ABSTRACT

BACKGROUND: Obstructive sleep apnoea (OSA) syndrome is a common disorder in the community. Association between hypertension and sleep apnoea and /or snoring has been described. The Berlin questionnaire is a validated instrument that is used to identify individuals who are at risk for OSA. The study aim to describe the prevalence of snoring and OSA among hypertensive subjects in South Western, Nigeria. METHODS: This was a descriptive study conducted at the Cardiology clinic of Ladoke Akintola University of Technology LAUTECH Teaching Hospital, Osogbo, South West Nigeria. One hundred consecutive hypertensive patients were recruited from the clinic. The Berlin questionnaire and the Epworth sleepiness scale (ESS) were used to determine excessive daytime sleepiness and the risk of having OSA. Statistical analysis was done using SPSS 16.0. Data were summarized as means ± S.D and percentages. RESULTS: The study participants consisted of 40 males (40.0%). The demographic data were similar between both genders except that females had higher mean body mass index than males. The prevalence of snoring was 50.0%. 52% were categorized as being at high risk of having OSA. Snorers were more likely to be older, males and to have a higher fasting blood sugar than non-snorers. 96% of snorers reported excessive daytime somnolence as predicted by the ESS score compared to 4% of non snorers. Prevalence of snoring was also higher among overweight and obese hypertensive subjects than normal body mass index hypertensive subjects. CONCLUSION: Snoring is common among hypertensive subjects in South Western Nigeria. Clinically suspected OSA was similarly high in prevalence among them. Early identification and management may reduce the cardiovascular risk of hypertensive subjects.


Subject(s)
Hypertension/epidemiology , Sleep Apnea, Obstructive/epidemiology , Snoring/epidemiology , Adult , Aged , Aged, 80 and over , Blood Pressure/physiology , Body Mass Index , Cross-Sectional Studies , Female , Humans , Hypertension/complications , Hypertension/diagnosis , Hypertension/physiopathology , Male , Middle Aged , Nigeria/epidemiology , Prevalence , Sleep Apnea, Obstructive/complications , Sleep Apnea, Obstructive/diagnosis , Sleep Apnea, Obstructive/physiopathology , Sleep Deprivation/diagnosis , Sleep Deprivation/epidemiology , Sleep Deprivation/etiology , Sleep Deprivation/physiopathology , Snoring/diagnosis , Snoring/etiology , Snoring/physiopathology
13.
Biol Psychiatry ; 72(5): 405-13, 2012 Sep 01.
Article in English | MEDLINE | ID: mdl-22537794

ABSTRACT

BACKGROUND: (±)-Modafinil has piqued interest as a treatment for attention-deficit/hyperactivity disorder and stimulant dependence. The R-enantiomer of modafinil might have unique pharmacological properties that should be further investigated. METHODS: (±)-Modafinil and its R-(-)- and S-(+)-enantiomers were synthesized and tested for inhibition of [(3)H] dopamine (DA) uptake and [(3)H]WIN 35428 binding in human dopamine transporter (DAT) wild-type and mutants with altered conformational equilibria. Data were compared with cocaine and the atypical DA uptake inhibitor, JHW 007. R- and S-modafinil were also evaluated in microdialysis studies in the mouse nucleus accumbens shell and in a cocaine discrimination procedure. RESULTS: (±)-, R-, and S-modafinil bind to the DAT and inhibit DA uptake less potently than cocaine, with R-modafinil having approximately threefold higher affinity than its S-enantiomer. Molecular docking studies revealed subtle differences in binding modes for the enantiomers. R-modafinil was significantly less potent in the DAT Y156F mutant compared with wild-type DAT, whereas S-modafinil was affected less. Studies with the Y335A DAT mutant showed that the R- and S-enantiomers tolerated the inward-facing conformation better than cocaine, which was further supported by [2-(trimethylammonium)ethyl]-methanethiosulfonate reactivity on the DAT E2C I159C. Microdialysis studies demonstrated that both R- and S-modafinil produced increases in extracellular DA concentrations in the nucleus accumbens shell less efficaciously than cocaine and with a longer duration of action. Both enantiomers fully substituted in mice trained to discriminate cocaine from saline. CONCLUSIONS: R-modafinil displays an in vitro profile different from cocaine. Future trials with R-modafinil as a substitute therapy with the potential benefit of cognitive enhancement for psychostimulant addiction are warranted.


Subject(s)
Benzhydryl Compounds/pharmacokinetics , Central Nervous System Stimulants/pharmacokinetics , Cocaine/pharmacokinetics , Dopamine Plasma Membrane Transport Proteins/antagonists & inhibitors , Dopamine Uptake Inhibitors/pharmacokinetics , Dopamine/metabolism , Animals , Benzhydryl Compounds/metabolism , Benzhydryl Compounds/therapeutic use , Central Nervous System Stimulants/metabolism , Cocaine/metabolism , Dopamine Plasma Membrane Transport Proteins/metabolism , Dopamine Uptake Inhibitors/metabolism , Dopamine Uptake Inhibitors/therapeutic use , Humans , Male , Mice , Microdialysis , Modafinil , Nucleus Accumbens/metabolism , Protein Binding , Substance-Related Disorders/drug therapy , Substance-Related Disorders/metabolism
14.
Chem Soc Rev ; 39(10): 3843-62, 2010 Oct.
Article in English | MEDLINE | ID: mdl-20820462

ABSTRACT

Anions cannot diffuse passively through biological membranes and membrane-bound proteins mainly govern the transmembrane movement of these charged species. The use of synthetic compounds that are able to facilitate the transmembrane transport of anions is a fascinating and burgeoning topic. The study of facilitated anion transport across lipid bilayers is an emerging field in supramolecular and bioorganic chemistry. In this critical review we describe the recent research progress in this area, focusing on literature published during the years 2007-2009. An overview of the assays that are used in the transmembrane transport of anions is also included (158 references).


Subject(s)
Anions/chemistry , Biological Transport , Calixarenes/chemistry , Cyclodextrins/chemistry , Fluorescent Dyes/chemistry , Ion-Selective Electrodes , Lipid Bilayers/metabolism , Peptides/chemistry
15.
ACS Med Chem Lett ; 2(1): 48-52, 2010 Oct 10.
Article in English | MEDLINE | ID: mdl-21344069

ABSTRACT

A series of modafinil (1) analogues was synthesized wherein 1) para-halo-substitutents were added to the aryl rings, 2) the sulfoxide function was removed, and 3) the primary amide group was replaced with secondary and tertiary amides and amines to investigate the effects of these chemical modifications on DAT, SERT and NET binding. In addition, the locomotor-stimulant effects in mice of (±)-modafinil (1), its R- and S-enantiomers and its para-chloro sulfinylacetamide analogue (5c) were compared to those of cocaine.

16.
Nat Chem ; 1(2): 138-44, 2009 May.
Article in English | MEDLINE | ID: mdl-21378827

ABSTRACT

Bicarbonate is involved in a wide range of biological processes, which include respiration, regulation of intracellular pH and fertilization. In this study we use a combination of NMR spectroscopy and ion-selective electrode techniques to show that the natural product prodigiosin, a tripyrrolic molecule produced by microorganisms such as Streptomyces and Serratia, facilitates chloride/bicarbonate exchange (antiport) across liposomal membranes. Higher concentrations of simple synthetic molecules based on a 4,6-dihydroxyisophthalamide core are also shown to facilitate this antiport process. Although it is well known that proteins regulate Cl(-)/HCO(3)(-) exchange in cells, these results suggest that small molecules may also be able to regulate the concentration of these anions in biological systems.


Subject(s)
Bicarbonates/chemistry , Chlorides/chemistry , Lipid Bilayers/chemistry , Liposomes/chemistry , Anions/chemistry , Ion Transport , Ion-Selective Electrodes , Magnetic Resonance Spectroscopy , Prodigiosin/chemistry
17.
Chem Commun (Camb) ; (30): 3246-8, 2006 Aug 14.
Article in English | MEDLINE | ID: mdl-17028758

ABSTRACT

The C3-symmetric triamide selectively transports NO3- anions across lipid vesicles: this H+-NO3- co-transporter alters the pH inside of liposomes experiencing a NO3-/Cl- gradient.


Subject(s)
Anions/chemistry , Chlorides/chemistry , Nitrates/chemistry , Crystallography, X-Ray , Hydrogen-Ion Concentration , Liposomes/chemistry , Models, Molecular , Molecular Structure
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