CP47,497-C8 and JWH073, commonly found in `Spice` herbal
... to be involved in tolerance to drugs of abuse such as THC (Wu et al., ...
... to be involved in tolerance to drugs of abuse such as THC (Wu et al., ...
Slide 1
... Lead optimization is the process in which a biologically active compound is modified to fulfill all the properties that are required from a drug (e.g. physicochemical and ADME/Tox properties). Pharmacophore can direct chemists to include/exclude specific chemical groups. ...
... Lead optimization is the process in which a biologically active compound is modified to fulfill all the properties that are required from a drug (e.g. physicochemical and ADME/Tox properties). Pharmacophore can direct chemists to include/exclude specific chemical groups. ...
VIEW PDF - Glaucoma Today
... I defined a new medication as one that was not yet available in all major countries. For sources, I used published articles, meeting abstracts, press releases, companies’ Web sites, and a clinical trial registry (http://www.clinicaltrials.gov). I also contacted senior management from worldwide ophth ...
... I defined a new medication as one that was not yet available in all major countries. For sources, I used published articles, meeting abstracts, press releases, companies’ Web sites, and a clinical trial registry (http://www.clinicaltrials.gov). I also contacted senior management from worldwide ophth ...
Problem 71- Vomiting, anorexia, nausea
... which helps to reverse the problem of endolymphatic hydrops. 2. Powerful antagonist effects at H3 receptors, and increases the levels of neurotransmitters released from the nerve endings. This explains the potent vasodilatory effects. Side-effects: headache, digestive-related side-effects. NB: In pr ...
... which helps to reverse the problem of endolymphatic hydrops. 2. Powerful antagonist effects at H3 receptors, and increases the levels of neurotransmitters released from the nerve endings. This explains the potent vasodilatory effects. Side-effects: headache, digestive-related side-effects. NB: In pr ...
GABA Receptors: Subtypes, Regional Distribution, and Function
... subunits, namely the α2, α3, and α5 subunits.21 The results of this study are supported by other studies that demonstrate that mice with this specific mutation in the α1 subunit fail to exhibit the sedative effect of benzodiazepines, but exhibit a normal anxiolytic response, equivalent to that of wi ...
... subunits, namely the α2, α3, and α5 subunits.21 The results of this study are supported by other studies that demonstrate that mice with this specific mutation in the α1 subunit fail to exhibit the sedative effect of benzodiazepines, but exhibit a normal anxiolytic response, equivalent to that of wi ...
Recent advances in knowledge about beta
... Although many such important concepts about beta-adrenergic receptors have been deduced from pharmacologic studies, the development and application of the biochemical approach to the study of beta-adrenergic receptors has initiated a new era of discovery concerning the intrinsic properties of these ...
... Although many such important concepts about beta-adrenergic receptors have been deduced from pharmacologic studies, the development and application of the biochemical approach to the study of beta-adrenergic receptors has initiated a new era of discovery concerning the intrinsic properties of these ...
DESIGNING OF POTENTIAL NEW ESTROGEN ANTAGONISTS FOR TREATMENT OF
... coronary heart disease, and more over cost of treatment is more as compared with the treatment of estrogen antagonist. Due to many other factors these drugs have decreased compliance in patient use. Among these estrogen antagonist like ethinylestradiol, in available preparations like Ovral-L and Nov ...
... coronary heart disease, and more over cost of treatment is more as compared with the treatment of estrogen antagonist. Due to many other factors these drugs have decreased compliance in patient use. Among these estrogen antagonist like ethinylestradiol, in available preparations like Ovral-L and Nov ...
- University of Mississippi
... as the basis for many studies regarding disease states. Currently, sigma-1 is hypothesized to play a very important role in addiction, pain, depression, Alzheimer’s disease, ...
... as the basis for many studies regarding disease states. Currently, sigma-1 is hypothesized to play a very important role in addiction, pain, depression, Alzheimer’s disease, ...
Long-Term Effects of Olanzapine, Risperidone, and Quetiapine on
... marrow toxicity, as well as excessive sedation and dosedependent risk of epileptic seizures (Baldessarini and Frankenburg, 1991). There is a keen interest in developing novel drugs with less adverse risk than clozapine but comparable antipsychotic effects. Several newer agents have emerged (Arnt and ...
... marrow toxicity, as well as excessive sedation and dosedependent risk of epileptic seizures (Baldessarini and Frankenburg, 1991). There is a keen interest in developing novel drugs with less adverse risk than clozapine but comparable antipsychotic effects. Several newer agents have emerged (Arnt and ...
The Design and Synthesis of Novel Antimicrobial Agents for Use in
... vivo to its active metabolite sulfanilamide (Figure 1.1).4 Prontosil was the first of the “sulfa” drugs discovered, and its discovery ushered in the era of antibiotics. Antibacterial agents, or antibiotics, are a class of a much larger group of compounds called antimicrobial agents. Antibiotics used ...
... vivo to its active metabolite sulfanilamide (Figure 1.1).4 Prontosil was the first of the “sulfa” drugs discovered, and its discovery ushered in the era of antibiotics. Antibacterial agents, or antibiotics, are a class of a much larger group of compounds called antimicrobial agents. Antibiotics used ...
No Slide Title
... A large number of analogues need to be synthesised to represent each different substituent and each different position of a substituent It is difficult to rationalise why specific substituents are good or bad for activity The effects of different substituents may not be additive (e.g. intramolecular ...
... A large number of analogues need to be synthesised to represent each different substituent and each different position of a substituent It is difficult to rationalise why specific substituents are good or bad for activity The effects of different substituents may not be additive (e.g. intramolecular ...
Anticoagulants, Thrombolytics Agents and Antiplatelet Drugs
... 1. Schafer AI. Am J Med 1996; 101: 199–209. ...
... 1. Schafer AI. Am J Med 1996; 101: 199–209. ...
DOA Detection Limits CHEM77
... human urine. These reagents are packaged specifically for use on a variety of AU® Clinical Chemistry Systems. The Emit® II Plus Opiate Assay detects morphine and morphine-3-glucuronide (the major metabolites of heroin) and codeine in human urine. Table 9 gives the compounds this assay detects and th ...
... human urine. These reagents are packaged specifically for use on a variety of AU® Clinical Chemistry Systems. The Emit® II Plus Opiate Assay detects morphine and morphine-3-glucuronide (the major metabolites of heroin) and codeine in human urine. Table 9 gives the compounds this assay detects and th ...
Opioid Receptor Imaging with Positron Emission Tomography and
... was used for PET imaging. Subjects were positioned so that transverse slices were acquired along the canthomeatal line. Before the study began, a physician placed an intra-arterial line in the radial artery of one arm and an intravenous line in the antecubital fossa of the other arm of the subject. ...
... was used for PET imaging. Subjects were positioned so that transverse slices were acquired along the canthomeatal line. Before the study began, a physician placed an intra-arterial line in the radial artery of one arm and an intravenous line in the antecubital fossa of the other arm of the subject. ...
Novartis Award for Hypertension Research Reconsidering the Roles
... progesterone receptor (PR)/androgen receptor (AR) subfamily of steroid hormone receptors from a common primordial ancestral protein.3 These studies and their implications for the basic biology of aldosterone action have been discussed elsewhere.4 The present review focuses on the clinical study (Ran ...
... progesterone receptor (PR)/androgen receptor (AR) subfamily of steroid hormone receptors from a common primordial ancestral protein.3 These studies and their implications for the basic biology of aldosterone action have been discussed elsewhere.4 The present review focuses on the clinical study (Ran ...
Gaba - American College of Neuropsychopharmacology
... (Fig. 12.4) (46). This group includes compounds called carbolines, some of which were isolated from biological tissues (47). However, neither the -carbolines nor any peptides have been demonstrated to act as biological ligands at benzodiazepine receptor sites (45). Surprisingly, some carbolines, ...
... (Fig. 12.4) (46). This group includes compounds called carbolines, some of which were isolated from biological tissues (47). However, neither the -carbolines nor any peptides have been demonstrated to act as biological ligands at benzodiazepine receptor sites (45). Surprisingly, some carbolines, ...
Adverse Reactions to Fluoroquinolones. An Overview on
... nervous system (CNS) and the skin are the most often observed adverse effects. Occasionally major events such as phototoxicity, cardiotoxicity, arthropathy and tendinitis occurr, leading to significant tolerability problems. Over the years, several structure-activity and side-effect relationships ha ...
... nervous system (CNS) and the skin are the most often observed adverse effects. Occasionally major events such as phototoxicity, cardiotoxicity, arthropathy and tendinitis occurr, leading to significant tolerability problems. Over the years, several structure-activity and side-effect relationships ha ...
A new, simple and robust radioligand binding method
... liquid and unbound ligand while retaining cells, including bound 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 attach ...
... liquid and unbound ligand while retaining cells, including bound 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 attach ...
Introduction to Fragment-Based Drug Discovery
... difficulty is that chemical bonds have strict length and geometric requirements, so if the two fragments are not perfectly positioned much of the potency gain expected will be lost due to strain in the linker [10, 11]. Therefore, a frequent alternative to fragment linking is fragment growing, as sho ...
... difficulty is that chemical bonds have strict length and geometric requirements, so if the two fragments are not perfectly positioned much of the potency gain expected will be lost due to strain in the linker [10, 11]. Therefore, a frequent alternative to fragment linking is fragment growing, as sho ...
Characterization of the Analgesic and Anti
... the following references: adenosine A1 (Lohse et al., 1987), A2 (Jarvis et al., 1989); a1-adrenergic (Greengrass and Bremner, 1979); a2adrenergic (Boyajian and Leslie, 1987); b-adrenergic (U’Prichard et al., 1978); calcitonin gene-related peptide (Yoshizaki et al., 1987); g-aminobutyric acidA, benzo ...
... the following references: adenosine A1 (Lohse et al., 1987), A2 (Jarvis et al., 1989); a1-adrenergic (Greengrass and Bremner, 1979); a2adrenergic (Boyajian and Leslie, 1987); b-adrenergic (U’Prichard et al., 1978); calcitonin gene-related peptide (Yoshizaki et al., 1987); g-aminobutyric acidA, benzo ...
EXPLORING THE EFFECTS OF NEWER THREE COMPONENT AMINOBENZYLATED REACTIONS OF TRIPHENYL IMIDAZOLE MOTIF AS POTENT ANTIMICROBIAL AND ANTIINFLAMMATORY
... measured. Along the test solution in each petridish, one cup was 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 antiinflam ...
... measured. Along the test solution in each petridish, one cup was 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 antiinflam ...
s - Clayton State University
... •A large number of analogues need to be synthesised to represent each different substituent and each different position of a substituent •It is difficult to rationalise why specific substituents are good or bad for activity •The effects of different substituents may not be additive ...
... •A large number of analogues need to be synthesised to represent each different substituent and each different position of a substituent •It is difficult to rationalise why specific substituents are good or bad for activity •The effects of different substituents may not be additive ...
The Role of Ligand Efficiency Measures in Drug Discovery
... and are summarised in Boxes 1-3; they can be applied at all stages of drug discovery, to evaluate fragments, screening hits, leads and candidate drugs. The use of molecular size, such as heavy atom count, in efficiency measures (see Box 1) has some caveats.29 Specifically, component atoms (C, N, O, ...
... and are summarised in Boxes 1-3; they can be applied at all stages of drug discovery, to evaluate fragments, screening hits, leads and candidate drugs. The use of molecular size, such as heavy atom count, in efficiency measures (see Box 1) has some caveats.29 Specifically, component atoms (C, N, O, ...
Naloxone fails to produce conditioned place aversion in
... regulating the `hedonic status' of the organism. The failure of NLX to induce aversion in MOR3/3 mice implies that NLX exerts its aversive e¡ect by blocking tonic activity of endogenous opioid ligands acting solely at the MOR since the total number and distribution of the DOR and U-opioid receptors ...
... regulating the `hedonic status' of the organism. The failure of NLX to induce aversion in MOR3/3 mice implies that NLX exerts its aversive e¡ect by blocking tonic activity of endogenous opioid ligands acting solely at the MOR since the total number and distribution of the DOR and U-opioid receptors ...
Hydrophobic interactions of phenoxazine modulators with bovine
... experiments. The experiments were performed on a 20 × 1⋅3 cm column of sephadexR G50 fine (Pharmacia) at 22°C, equilibrated with standard buffer solution. The flow rate was maintained at 25 ml/h. BSA solution (20 ml, 1%) containing 1⋅0 × 10–4 M phenoxazine modulator, after incubation at 37°C for 6 h ...
... experiments. The experiments were performed on a 20 × 1⋅3 cm column of sephadexR G50 fine (Pharmacia) at 22°C, equilibrated with standard buffer solution. The flow rate was maintained at 25 ml/h. BSA solution (20 ml, 1%) containing 1⋅0 × 10–4 M phenoxazine modulator, after incubation at 37°C for 6 h ...
CCR5 receptor antagonist
CCR5 receptor antagonists are a class of small molecules that antagonize the CCR5 receptor. The C-C motif chemokine receptor CCR5 is involved in the process by which HIV, the virus that causes AIDS, enters cells. Hence antagonists of this receptor are entry inhibitors and have potential therapeutic applications in the treatment of HIV infections.The life cycle of the HIV presents potential targets for drug therapy, one of them being the viral entry pathway. The C-C motif chemokine receptors CCR5 and CXCR4 are the main chemokine receptors involved in the HIV entry process. These receptors belong to the seven transmembrane G-protein-coupled receptor (GPCR) family and are predominantly expressed on human T-cells, dendritic cells and macrophages, Langerhans cells. They play an important role as co-receptors that HIV type 1 (HIV-1) uses to attach to cells before viral fusion and entry into host cells. HIV isolates can be divided into R5 and X4 strains. R5 strain is when the virus uses the co-receptor CCR5 and X4 strain is when it uses CXCR4. The location of CCR5 receptors at the cell surface, both large and small molecules have the potential to interfere with the CCR5-viral interaction and inhibit viral entry into human cells.