Hit discovery and hit-to-lead approaches
... chemistry program. For novel targets, focused- and fragmentbased screening would also become the method of choice, if no suitable high-throughput assay can be developed for HTS. Novel ideas generated by information on small molecules reported in the literature are potentially the fastest entry to ne ...
... chemistry program. For novel targets, focused- and fragmentbased screening would also become the method of choice, if no suitable high-throughput assay can be developed for HTS. Novel ideas generated by information on small molecules reported in the literature are potentially the fastest entry to ne ...
Anti-Parkinsonism drugs
... 6. Drugs e.g. DA2 receptors blockers , rarely by alpha-methyldopa, or large doses of reserpine ...
... 6. Drugs e.g. DA2 receptors blockers , rarely by alpha-methyldopa, or large doses of reserpine ...
Left heart failure
... The clinical picture in heart failure consists of: • signs (the objective manifestations of depressed cardiac performance), • symptoms (abnormalities perceived by the patient). Left heart failure: is a "forward failure" - reduced ejection, "backward failure" - rise in pulmonary capillary pressure. S ...
... The clinical picture in heart failure consists of: • signs (the objective manifestations of depressed cardiac performance), • symptoms (abnormalities perceived by the patient). Left heart failure: is a "forward failure" - reduced ejection, "backward failure" - rise in pulmonary capillary pressure. S ...
Agonist vs Antagonist
... response Effective in preventing LH surge Reduction of hyper-stimulation ...
... response Effective in preventing LH surge Reduction of hyper-stimulation ...
Neuropharmacology of Aggressive Behavior - E
... agonists in the antiaggressive dose-ranges have dual effects on serotoninergic neurotransmission: by acting at the autoreceptors, they very effectively inhibit 5-HT neurotransmission. In contrast, when acting directly at postsynaptic sites, these agonists mimics the effect of 5-HT released, thereby ...
... agonists in the antiaggressive dose-ranges have dual effects on serotoninergic neurotransmission: by acting at the autoreceptors, they very effectively inhibit 5-HT neurotransmission. In contrast, when acting directly at postsynaptic sites, these agonists mimics the effect of 5-HT released, thereby ...
Master Thesis 2016 - 2017 - Department of Drug Design and
... The time is nearing when you have to decide on your Master Project. Maybe you have known for a long time in which area you want to do your project, maybe you enjoy several fields, and have not yet made up your mind. I hope you will find inspiration in this catalogue to help guide you to the right pr ...
... The time is nearing when you have to decide on your Master Project. Maybe you have known for a long time in which area you want to do your project, maybe you enjoy several fields, and have not yet made up your mind. I hope you will find inspiration in this catalogue to help guide you to the right pr ...
Hallucinogens - public.coe.edu
... Hofmann took lysergic acid from ergot alkaloids and combined it with other compounds. o ...
... Hofmann took lysergic acid from ergot alkaloids and combined it with other compounds. o ...
MANAGEMENT OF POSTOPERATIVE NAUSEA AND VOMITING
... peptide activity is tied to at least three G-protein-coupled receptor subtypes found in the peripheral or central nervous tissue: neurokinin receptor subtype 1 (NK1), type 2 (NK2), and subtype 3 (NK3). The NK1 receptors are located in the area postrema and are thought to play a particularly importan ...
... peptide activity is tied to at least three G-protein-coupled receptor subtypes found in the peripheral or central nervous tissue: neurokinin receptor subtype 1 (NK1), type 2 (NK2), and subtype 3 (NK3). The NK1 receptors are located in the area postrema and are thought to play a particularly importan ...
Drug and Active Principle:
... blockade caused by non-depolarizing muscle relaxants. 4. As antidote in poisoning with parasympatholytic drugs because it has access to AChE in the brain (physostigmine). 5. In the treatment of glaucoma (neostigmine, pyridostigmine, physostigmine pilocarpine paraoxon and ecothiopate): however, their ...
... blockade caused by non-depolarizing muscle relaxants. 4. As antidote in poisoning with parasympatholytic drugs because it has access to AChE in the brain (physostigmine). 5. In the treatment of glaucoma (neostigmine, pyridostigmine, physostigmine pilocarpine paraoxon and ecothiopate): however, their ...
Pharmacology
... = thus interfering with AV conducn in arterial tachycardias, and to slow ventricular rate. ...
... = thus interfering with AV conducn in arterial tachycardias, and to slow ventricular rate. ...
REVIEW ARTICLE Modulation of b-adrenergic receptor subtype activities in
... recently for the b2- but not the b1-AR.261 This model also explains the inability of some b-AAs with pronounced neutral antagonism to block the effects of receptor overexpression fully, as neutral antagonists counteract activation by endogenous catecholamines but not activation by spontaneous transi ...
... recently for the b2- but not the b1-AR.261 This model also explains the inability of some b-AAs with pronounced neutral antagonism to block the effects of receptor overexpression fully, as neutral antagonists counteract activation by endogenous catecholamines but not activation by spontaneous transi ...
Cannabinoids and the skeleton: From marijuana to reversal of bone
... anandamide concentrations have been attributed to low substrate (arachidonic acid esterified at the 1-position) levels for this pathway and/or the short anandamide half-life in vivo (t1/2 B5 min) (52,53). Anandamide is biosynthesized through N-acyl phosphatidyl ethanolamine phospholipase D (NAPEPLD) ...
... anandamide concentrations have been attributed to low substrate (arachidonic acid esterified at the 1-position) levels for this pathway and/or the short anandamide half-life in vivo (t1/2 B5 min) (52,53). Anandamide is biosynthesized through N-acyl phosphatidyl ethanolamine phospholipase D (NAPEPLD) ...
CELL MODEL SYSTEMS IN CHARACTERIZING α2
... The three 2-adrenoceptor (2-AR) subtypes belong to the G protein-coupled receptor superfamily and represent potential drug targets. These receptors have many vital physiological functions, but their actions are complex and often oppose each other. Current research is therefore driven towards disco ...
... The three 2-adrenoceptor (2-AR) subtypes belong to the G protein-coupled receptor superfamily and represent potential drug targets. These receptors have many vital physiological functions, but their actions are complex and often oppose each other. Current research is therefore driven towards disco ...
Full text - FNWI (Science) Education Service Centre
... pain after CNS dysfunction, and not before. In general, the mechanism of migraine attack is believed to consist of four steps after CNS dysfunction: 1) A local vasodilatation of the intracranial extracerebral blood vessels / meningeal blood vessel promoted by specific triggers. 2) Stimulation of pai ...
... pain after CNS dysfunction, and not before. In general, the mechanism of migraine attack is believed to consist of four steps after CNS dysfunction: 1) A local vasodilatation of the intracranial extracerebral blood vessels / meningeal blood vessel promoted by specific triggers. 2) Stimulation of pai ...
Review Drug chirality: a consideration of the significance
... (Blaschke et al., 1979). Thus, if the drug had been used as a single isomer then the tragedy of the early 1960s could have been avoided. However, some older data obtained with a more sensitive test species, New Zealand White rabbits, indicates that both enantiomers of the drug are teratogenic (Fabro ...
... (Blaschke et al., 1979). Thus, if the drug had been used as a single isomer then the tragedy of the early 1960s could have been avoided. However, some older data obtained with a more sensitive test species, New Zealand White rabbits, indicates that both enantiomers of the drug are teratogenic (Fabro ...
Versatile Oligo(N-Substituted) Glycines: The
... of treating HIV infection [1]. Several peptoids, similar in sequence to Tat49±57, have been synthesized with the intention of preventing the HIV-Tat/Tar interaction, and thus preventing HIV replication [24, 25, 30, 31]. However, only recently has this class of peptoids been applied to membrane trans ...
... of treating HIV infection [1]. Several peptoids, similar in sequence to Tat49±57, have been synthesized with the intention of preventing the HIV-Tat/Tar interaction, and thus preventing HIV replication [24, 25, 30, 31]. However, only recently has this class of peptoids been applied to membrane trans ...
(12)Indian Patent Application ______________________________________________________________
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
... provide an effective therapeutic treatment in immune-mediated diseases, e.g. intestinal disorders, such as autoimmune and inflammatory diseases or conditions. T lymphocyte (T cell) infiltration into the small intestine and colon has been linked specifically to the pathogenesis of Coeliac diseases, f ...
Karen R. Hurd Submitted in partial fulfillment of requirements
... Step 2: A concentrated acid (HCl) is used to remove the CH3 from the oxygen attached to the ring. This is done by Cl- that attacks the carbon. The electrons are pushed onto the ring, making the ring with the oxygen and the ring’s other substituents a good leaving group. H+ ion protonates the OH grou ...
... Step 2: A concentrated acid (HCl) is used to remove the CH3 from the oxygen attached to the ring. This is done by Cl- that attacks the carbon. The electrons are pushed onto the ring, making the ring with the oxygen and the ring’s other substituents a good leaving group. H+ ion protonates the OH grou ...
A. Glucocorticoid drugs
... carditis, rhumatic arthritis, rheumatoid arthritis, osteoarthritis, systemic lupus erythematosus, polyarthritis nodosa, nephritic syndrome, etc. ...
... carditis, rhumatic arthritis, rheumatoid arthritis, osteoarthritis, systemic lupus erythematosus, polyarthritis nodosa, nephritic syndrome, etc. ...
Straight Tox 2C phenethylamines
... To see a world in a grain of sand, And a heaven in a wild flower, Hold infinity in the palm of your hand, And eternity in an hour. _ William Blake I found this opening stanza from William Blake’s poem Auguries of Innocence, while looking for some clever way to use the letters “2C” as the words “to s ...
... To see a world in a grain of sand, And a heaven in a wild flower, Hold infinity in the palm of your hand, And eternity in an hour. _ William Blake I found this opening stanza from William Blake’s poem Auguries of Innocence, while looking for some clever way to use the letters “2C” as the words “to s ...
Pharmacology
... Pharmacology is an experimental science, of which the theory is obtained from the experimental studies, including nonclinical and clinical study. It is the experimental studies that accumulate the rich content of pharmacology, and promote the development of modern pharmacology. This is why experimen ...
... Pharmacology is an experimental science, of which the theory is obtained from the experimental studies, including nonclinical and clinical study. It is the experimental studies that accumulate the rich content of pharmacology, and promote the development of modern pharmacology. This is why experimen ...
6 Synergy and polyvalence: paradigms to explain the activity of herbal products
... but a useful definition is ‘an effect seen by a combination of substances that is greater than would have been expected from a consideration of individual contributions’ (Heinrich et al., 2004). More precise definitions, incorporating mathematical considerations, have been discussed by Berenbaum (19 ...
... but a useful definition is ‘an effect seen by a combination of substances that is greater than would have been expected from a consideration of individual contributions’ (Heinrich et al., 2004). More precise definitions, incorporating mathematical considerations, have been discussed by Berenbaum (19 ...
Neurotransmitters in alcoholism: A review of neurobiological and
... alcohol exposure causes a drop in the extra cellular glutamate levels in a region of the brain called striatum which contains the nucleus accumbens and other structures.[25] Glutamate mediated signal transmission is suppressed in the central nucleus of the amygdala following acute administration and ...
... alcohol exposure causes a drop in the extra cellular glutamate levels in a region of the brain called striatum which contains the nucleus accumbens and other structures.[25] Glutamate mediated signal transmission is suppressed in the central nucleus of the amygdala following acute administration and ...