Drugs online research references
J Med Chem. 1999 Aug 12;42(16):3101-8.
Synthesis and characterization of fluorescent ligands for the norepinephrine transporter: potential neuroblastoma imaging agents.
Hadrich D, Berthold F, Steckhan E, Bonisch H.
Kekule-Institut fur Organische Chemie und Biochemie, Universitat Bonn, Gerhard-Domagk-Strasse 1, D-53121 Bonn, Germany.
Radiolabeled m-iodobenzylguanidine (MIBG) is a tumor-seeking radioactive drug used in the diagnosis and treatment of pheochromocytomas and neuroblastomas. It is transported into the tumor cells by the neuronal norepinephrine (NE) transporter (NET) which is expressed in almost all neuroblastoma cells. Here, we describe the synthesis and some pharmacological properties of a series of fluorescent compounds structurally related to the NET substrate, MIBG, or to the NET inhibitors, (-)-(2R,3S)-cocaine and nisoxetine. Three of 10 synthesized fluorescent compounds, 1-(1-naphthylmethyl)guanidinium sulfate (1), 1-[2-(dibenz[b, f]azepin-5-yl)ethyl]guanidinium sulfate (2), and (2R, 3S)-2beta-ethoxycarbonyl-3beta-tropanyl 5-(dimethylamino)naphthalene-1-sulfonate (6), exhibited high affinity (IC(50) about 50 nM) for the NET. The nisoxetine derivatives 8 (rac-N-[(3-methylamino-1-phenyl)propyl]-5-(dimethylamino)-1-naphthale nesulfonamide) and 9 (rac-4-[(3-methylamino-1-phenyl)propyl]amino-7-nitro-2,1, 3-benzoxadiazole) and especially the guanidine derivative 4 (1-[4-(4-phenyl-1,3-butadienyl)benzyl]guanidinium sulfate) which are characterized by intermediate affinity for the NET (IC(50) 370-850 nM) caused significant and nisoxetine-sensitive cell fluorescence. At least the guanidine derivative 4 might represent a potentially useful agent for imaging of neuroblastoma cells.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10447954&dopt=Abstract
note: kwd match prozac online literature
Indian J Exp Biol. 2002 Nov;40(11):1240-4.
Role of antioxidants in chronic fatigue syndrome in mice.
Singh A, Garg V, Gupta S, Kulkarni SK.
Pharmacology Division, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160 014, India.
The present study was carried out using mice model of chronic fatigue syndrome (CFS) in which mice were forced to swim everyday for 7 days for a 6 min session. There was a significant increase in despair behavior (immobility period) in saline treated mice on successive days. Treatment with potent antioxidants carvedilol (5 mg/kg, i.p.) and melatonin (10 mg/kg, i.p.) produced a significant reduction in immobility period. Similar results were observed with herbal products St. John's Wort (Hypericum perforatum L) (10 mg/kg, p.o.) and GS-02 (20 mg/kg, p.o.). Fluoxetine, a selective serotonin reuptake inhibitor produced a significant effect only on first and second day of its treatment. Biochemical analysis revealed that chronic swim test significantly increased lipid peroxidation and catalase levels in whole brains of mice. There was a decrease in the levels of super oxide dismutase (SOD) and glutathione reductase (GSH) in the brain. Administration of carvedilol, melatonin, GS-02 and St. John's Wort restored the levels of lipid peroxidation and glutathione. The enzymes SOD and catalase were also restored. Fluoxetine affected the biochemical variables not to the same extent as other treatments. The findings of the present study suggest that oxidative stress might play a significant role in the pathophysiology of CFS. Thus antioxidants and herbal products like St. Johns wort and GS-02 could be useful in the treatment of CFS.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=13677625&dopt=Abstract
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J Pharm Pharmacol. 1999 Jun;51(6):741-3.
Effect of some antidepressants on glycaemia and insulin levels of normoglycaemic and alloxan-induced hyperglycaemic mice.
Erenmemisoglu A, Ozdogan UK, Saraymen R, Tutus A.
Department of Nuclear Medicine, Erciyes University, Kayseri, Turkey.
Depression is an important problem among diabetic patients. We have investigated the effect of some antidepressant drugs on plasma glucose and insulin levels in normoglycaemic and alloxan-induced diabetic mice. For this purpose the effects of nortryptiline (as an example of a tricyclic antidepressant) and fluoxetine and sertraline (as examples of selective 5-HT re-uptake inhibitors) were examined on plasma glucose and insulin levels. Nortryptiline significantly increased glucose levels and reduced insulin levels in all animals. Although neither fluoxetine nor sertraline induced changes in insulin levels, both significantly reduced the blood glucose levels of mice. These results suggest that antidepressive treatment has important risks particularly for diabetics. Tricyclic antidepressants might induce an important decrease in glucose tolerance and worsen the control of diabetic patients. Selective 5-HT re-uptake inhibitors, on the other hand, might reduce plasma glucose independently of insulin levels. This point is particularly important and should be remembered when insulin or oral antidiabetic agents are administered to diabetics, because of the possible risk of hypoglycaemia.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10454053&dopt=Abstract
note: kwd match prozac online literature
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