Antidepressant specificity of serotonin transporter suggested by three LeuT–SSRI structures Zheng Zhou
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
... lower affinity than to their principal target, SERT3,4. The selectivity of SSRIs for SERT is intriguing. Merely one or two different functional group substitutions are sufficient to convert an SSRI into a norepinephrine-reuptake inhibitor (NRI) with higher affinity to NET5–7. It is recognized that b ...
Rifampicin Antagonizes the Effect of Chloroquine on Chloroquine
... Pgh1 and therefore decreasing CQ accumulation inside the food vacuole. However, this postulation is unable to explain how verapamil and other reversal agents are able to increase CQ inside the food vacuole and counter resistance. Another factor to consider is the fact that RIF is a known CYP3A4 indu ...
... Pgh1 and therefore decreasing CQ accumulation inside the food vacuole. However, this postulation is unable to explain how verapamil and other reversal agents are able to increase CQ inside the food vacuole and counter resistance. Another factor to consider is the fact that RIF is a known CYP3A4 indu ...
Kitonde et al., Afr J Tradit Complement Altern Med. (2013) 10 (1):000
... used. Two fold serial dilutions were prepared from each stock solution. Paper discs were punched from Whatman filter paper No.1 using a paper punch. From each concentration prepared, 100µl were pipetted onto individually placed sterile paper discs (0.6cm) on flat-bottomed glass plates drop by drop u ...
... used. Two fold serial dilutions were prepared from each stock solution. Paper discs were punched from Whatman filter paper No.1 using a paper punch. From each concentration prepared, 100µl were pipetted onto individually placed sterile paper discs (0.6cm) on flat-bottomed glass plates drop by drop u ...
A new, simple and robust radioligand binding method
... ligand, attached to the bottom surface. Immediately, 300 μl of binding buffer (including about 2 nM [3H]-RX821002) was added rather forcefully to the cells. Thereby, most of the HEK293 cells became re-suspended, due to that cell attachment was weak since attachment of the cells had been achieved jus ...
... ligand, attached to the bottom surface. Immediately, 300 μl of binding buffer (including about 2 nM [3H]-RX821002) was added rather forcefully to the cells. Thereby, most of the HEK293 cells became re-suspended, due to that cell attachment was weak since attachment of the cells had been achieved jus ...
EXPLORING THE EFFECTS OF NEWER THREE COMPONENT AMINOBENZYLATED REACTIONS OF TRIPHENYL IMIDAZOLE MOTIF AS POTENT ANTIMICROBIAL AND ANTIINFLAMMATORY
... filled with solvent which acted as control. The antifungal activity of compounds was compared with a standard drug Griseofulvin. The results of antimicrobial profile were depicted in Table 2. In vitro antiinflammatory activity The invitro anti‐inflammatory activity was evaluated by ...
... filled with solvent which acted as control. The antifungal activity of compounds was compared with a standard drug Griseofulvin. The results of antimicrobial profile were depicted in Table 2. In vitro antiinflammatory activity The invitro anti‐inflammatory activity was evaluated by ...
Pharmacogenetic studies of paclitaxel in ovarian cancer pharmacodynamics and
... combination with carboplatin after initial cytoreductive surgery. The response to treatment and the severity of adverse drug reactions after chemotherapy varies greatly among individuals, and one of the most important factors responsible for these differences is now recognized to be the genetic vari ...
... combination with carboplatin after initial cytoreductive surgery. The response to treatment and the severity of adverse drug reactions after chemotherapy varies greatly among individuals, and one of the most important factors responsible for these differences is now recognized to be the genetic vari ...
fluphenazine and perphenazine impact on melanogenesis and
... Abstract: Fluphenazine and perphenazine as a phenothiazine-class antipsychotic drugs are widely used to treat psychoses and schizophrenia, however their use is associated with significant side effects such as extrapyramidal symptoms as well as ocular and skin disorders. The aim of this study was to ...
... Abstract: Fluphenazine and perphenazine as a phenothiazine-class antipsychotic drugs are widely used to treat psychoses and schizophrenia, however their use is associated with significant side effects such as extrapyramidal symptoms as well as ocular and skin disorders. The aim of this study was to ...
DENS 521 4th S
... Fourth-generation agents are particularly useful for the empirical treatment of serious infections in hospitalized patients when gram-positive microorganisms, Enterobacteriaceae, and Pseudomonas all are potential etiologies ...
... Fourth-generation agents are particularly useful for the empirical treatment of serious infections in hospitalized patients when gram-positive microorganisms, Enterobacteriaceae, and Pseudomonas all are potential etiologies ...
Allosteric Modulation: a Novel Approach to Drug Discovery
... The Ability to Discover Small Molecule Drugs for GPCR Targets That Historically have Evaded Small Molecule Drug Developers Several GPCR targets are currently thought to be beyond the reach of conventional competitive drug discovery approaches due to the complexity of the interaction of the endogenou ...
... The Ability to Discover Small Molecule Drugs for GPCR Targets That Historically have Evaded Small Molecule Drug Developers Several GPCR targets are currently thought to be beyond the reach of conventional competitive drug discovery approaches due to the complexity of the interaction of the endogenou ...
Pharmacology Objectives 12
... pentasaccharide complex to antithrombin resulting in a conformational change that increases the inhibition of factor Xa, but only the longer chains of UFH can bind both antithrombin and prothrombin to form a prothrombin ternary complex. Therefore, UFH has equal affect on factors Xa and IIa while LMW ...
... pentasaccharide complex to antithrombin resulting in a conformational change that increases the inhibition of factor Xa, but only the longer chains of UFH can bind both antithrombin and prothrombin to form a prothrombin ternary complex. Therefore, UFH has equal affect on factors Xa and IIa while LMW ...
Meiosis and sexual life cycles - March 23
... Possibility 1 Two equally probable arrangements of chromosomes at metaphase I ...
... Possibility 1 Two equally probable arrangements of chromosomes at metaphase I ...
Bioisosterism: A Rational Approach in Drug Design
... instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and to correlate these values to the observed biological activity. Thus, an additional objective of this review was to demonstrate the opportunities that one has in employing bioisosteres to gain more specif ...
... instances, physicochemical effects such as electronegativity, steric size, and lipophilicity and to correlate these values to the observed biological activity. Thus, an additional objective of this review was to demonstrate the opportunities that one has in employing bioisosteres to gain more specif ...
Pharmacological Evaluation of Saraca indica Leaves for Central
... indica leaves extracted successively with petroleum ether, chloroform, methanol and water respectively depending upon their polarity. CNS depressant activity was evaluated using pentobarbitone induced sleeping time and by determining locomotor activity using actophotometer. Methanolic extract of Sar ...
... indica leaves extracted successively with petroleum ether, chloroform, methanol and water respectively depending upon their polarity. CNS depressant activity was evaluated using pentobarbitone induced sleeping time and by determining locomotor activity using actophotometer. Methanolic extract of Sar ...
Protein Binding Drug-Drug Interaction between Warfarin and
... to albumins and, most probably, competed for the same binding site of the protein. Albumins have two main drug binding sites characterized as Sudlow site I and Sudlow site II [8]. These sites bind drugs selectively. Warfarin primarily binds to the site I [9,10]. Because tizoxanide displaced warfarin ...
... to albumins and, most probably, competed for the same binding site of the protein. Albumins have two main drug binding sites characterized as Sudlow site I and Sudlow site II [8]. These sites bind drugs selectively. Warfarin primarily binds to the site I [9,10]. Because tizoxanide displaced warfarin ...
Vinorelbine - BC Cancer Agency
... Vinorelbine is a semisynthetic vinca alkaloid derived from vinblastine. Vinca alkaloids such as vincristine and ...
... Vinorelbine is a semisynthetic vinca alkaloid derived from vinblastine. Vinca alkaloids such as vincristine and ...
Covalent inhibitors in drug discovery: from accidental discoveries to
... Advantages of covalent drugs Unacceptable toxicity and insufficient efficacy are frequently cited reasons for the attrition of drug candidates during large-scale clinical trials [31]. While pharmaceutical teams continue to hedge against attrition by careful target and patient selection [32], the mai ...
... Advantages of covalent drugs Unacceptable toxicity and insufficient efficacy are frequently cited reasons for the attrition of drug candidates during large-scale clinical trials [31]. While pharmaceutical teams continue to hedge against attrition by careful target and patient selection [32], the mai ...
- The University of Liverpool Repository
... As highlighted by Denning and Bromley (23), the antifungal pipeline has failed to produce new antifungal drugs with mechanisms of action different to existing classes since caspofungin was licensed in 2001. Many potential antifungal targets have been investigated but translating these early stage p ...
... As highlighted by Denning and Bromley (23), the antifungal pipeline has failed to produce new antifungal drugs with mechanisms of action different to existing classes since caspofungin was licensed in 2001. Many potential antifungal targets have been investigated but translating these early stage p ...
Antifungal drugs and resistance: Current concepts
... of the azole family and Pramiconazole is another new member of triazole class in the stages of development for the treatment of superficial infections caused by dermatophytes, yeasts and many other fungi [37]. ...
... of the azole family and Pramiconazole is another new member of triazole class in the stages of development for the treatment of superficial infections caused by dermatophytes, yeasts and many other fungi [37]. ...
International Journal of Pharmaceutical Sciences and Drug Research 2014; 6(4): 329-333
... employed to determine the antibacterial activities. About 0.2 ml of the standardized 24 hour old broth culture of the test organisms were spread onto sterile Muller Hinton Agar plates. These were then allowed to set. With the aid of a sterile cork borer, wells of about 6 mm in diameter were bored on ...
... employed to determine the antibacterial activities. About 0.2 ml of the standardized 24 hour old broth culture of the test organisms were spread onto sterile Muller Hinton Agar plates. These were then allowed to set. With the aid of a sterile cork borer, wells of about 6 mm in diameter were bored on ...
Poster martinive AACR2006
... Philippe Martinive1, Julie DeWever1, Caroline Bouzin1, Pierre Sonveaux1, Christine ...
... Philippe Martinive1, Julie DeWever1, Caroline Bouzin1, Pierre Sonveaux1, Christine ...
Document
... Colchicine toxicity is based on it is antimitotic activity that it binds to cell protein tubulin (Tubuline works like a receptor for colchicine) and inhibits mitosis in metaphase by blocks spindle formation by disrupting microtubules [16]. Characteristically colchicine have a short half-life in the ...
... Colchicine toxicity is based on it is antimitotic activity that it binds to cell protein tubulin (Tubuline works like a receptor for colchicine) and inhibits mitosis in metaphase by blocks spindle formation by disrupting microtubules [16]. Characteristically colchicine have a short half-life in the ...
Quinoline and Iso Quinoline alkaloids
... Emetine (methyl cephaline) is antiamebic Emetine is more expectorant and less emetic in action than cephaeline , and is added to many cough medicines. Psychotrine and its O-methyl ether are selective inhibitors of human immunodeficiency virus and their study could lead to the development of therapeu ...
... Emetine (methyl cephaline) is antiamebic Emetine is more expectorant and less emetic in action than cephaeline , and is added to many cough medicines. Psychotrine and its O-methyl ether are selective inhibitors of human immunodeficiency virus and their study could lead to the development of therapeu ...
Coadministration of Oral Cyclosporin A Enables Oral Therapy with
... a single agent at a dose of 60 mg/m2 during course 1 and paclitaxel i.v. at a dose of 175 mg/m2 administered as a 3-h infusion during course 2. In the second part of the study, it was planned that eight evaluable patients would receive paclitaxel on two randomized occasions. On one occasion, they wo ...
... a single agent at a dose of 60 mg/m2 during course 1 and paclitaxel i.v. at a dose of 175 mg/m2 administered as a 3-h infusion during course 2. In the second part of the study, it was planned that eight evaluable patients would receive paclitaxel on two randomized occasions. On one occasion, they wo ...
Bioinformatics (2011) 27
... the ADME (absorption, distribution, metabolism, and excretion) profile. Due to the continuous demand to investigate HSA binding properties of novel drugs, drug candidates and drug-like compounds, a support vector machine (SVM) model was developed that efficiently predicts albumin binding. Our SVM mo ...
... the ADME (absorption, distribution, metabolism, and excretion) profile. Due to the continuous demand to investigate HSA binding properties of novel drugs, drug candidates and drug-like compounds, a support vector machine (SVM) model was developed that efficiently predicts albumin binding. Our SVM mo ...
ANALGESIC AND ANTHELMINTIC ACTIVITY OF VARIOUS EXTRACTS OF ANDROGRAPHIS Research Article
... analgesiometer (Techno, India). The magnitude of the current which was passing through the naked nichrome wire was kept constant at 6 ampere. The tail skin was kept at a distance of 1.5 cm from the heat source. The radiant heat (55±2 °C) in the tail was applied and maintained at 2.5 cm measured from ...
... analgesiometer (Techno, India). The magnitude of the current which was passing through the naked nichrome wire was kept constant at 6 ampere. The tail skin was kept at a distance of 1.5 cm from the heat source. The radiant heat (55±2 °C) in the tail was applied and maintained at 2.5 cm measured from ...