Bez nadpisu - Univerzita Karlova
... attacks, an observation that strengthens the association of serotonin abnormalities with these headache syndromes. At present it is available only for parenteral injection, unlike the ergot antimigraine medications, which are available for oral and rectal (suppository) use. A number of important ant ...
... attacks, an observation that strengthens the association of serotonin abnormalities with these headache syndromes. At present it is available only for parenteral injection, unlike the ergot antimigraine medications, which are available for oral and rectal (suppository) use. A number of important ant ...
Alcohol antagonists - MIT OpenCourseWare
... Like naltrexone, Haldol is a selective alcohol antagonist. Haldol does not block most of the effects of ethanol, and it will actually increase the level of drowsiness. However, Haldol selectively blocks the effect of ethanol on the wanting pathway. Dopamine antagonists can prevent a rat from learnin ...
... Like naltrexone, Haldol is a selective alcohol antagonist. Haldol does not block most of the effects of ethanol, and it will actually increase the level of drowsiness. However, Haldol selectively blocks the effect of ethanol on the wanting pathway. Dopamine antagonists can prevent a rat from learnin ...
Sympatholytics
... Tachycardia (α1-selective produce less tachycardia because they do not increase NA release from sympathetic nerve terminal) ...
... Tachycardia (α1-selective produce less tachycardia because they do not increase NA release from sympathetic nerve terminal) ...
d) Bronchodilator Response
... The autonomic system is generally considered an efferent system, where impulses travel from the brain and spinal cord out to the various neuroeffector sites. Three different efferent nervous pathways supply the airway smooth muscle: cholinergic, adrenergic and non adrenergic non cholinergic (NANC). ...
... The autonomic system is generally considered an efferent system, where impulses travel from the brain and spinal cord out to the various neuroeffector sites. Three different efferent nervous pathways supply the airway smooth muscle: cholinergic, adrenergic and non adrenergic non cholinergic (NANC). ...
Drug Receptors
... the capability to produce distinctly different pharmacologic effects. Some of these effects could be beneficial, some could be toxic. Such a drug would be said to be a selective. The factors that determine which particular effect of a drug will be observed are the affinity and intrinsic activity of ...
... the capability to produce distinctly different pharmacologic effects. Some of these effects could be beneficial, some could be toxic. Such a drug would be said to be a selective. The factors that determine which particular effect of a drug will be observed are the affinity and intrinsic activity of ...
DOSE *RESPONSE CURVES
... Full Agonists: Compounds that are able to elicit a maximal response following receptor occupation and activation. Partial Agonists: Compounds that can activate receptors but are unable to elicit the maximal response of the receptor system. Inverse agonist: an agent which binds to the same receptor b ...
... Full Agonists: Compounds that are able to elicit a maximal response following receptor occupation and activation. Partial Agonists: Compounds that can activate receptors but are unable to elicit the maximal response of the receptor system. Inverse agonist: an agent which binds to the same receptor b ...
The Carlat Psychiatry Report ROZEREM (ramelteon) Fact Sheet
... • Appears to cause little in the way of next day fatigue or other impairment. • Abuse potential: One company-sponsored study showed that 14 patients with a history of drug abuse rated Rozerem as no more abusable than placebo. • Increases serum prolactin in women by an average of 34%. • Pregnancy Cat ...
... • Appears to cause little in the way of next day fatigue or other impairment. • Abuse potential: One company-sponsored study showed that 14 patients with a history of drug abuse rated Rozerem as no more abusable than placebo. • Increases serum prolactin in women by an average of 34%. • Pregnancy Cat ...
Week 6 lecture slides
... interfere with ethanol binding, but Ro 154513 does interfere with ethanol binding because of this bulky azido group that displaces ethanol. In vitro, Ro 15-4513 competitively inhibits ethanol binding to the GABAA receptor complex. In vivo, Ro 154513 inhibits the sedation caused by alcohol but does n ...
... interfere with ethanol binding, but Ro 154513 does interfere with ethanol binding because of this bulky azido group that displaces ethanol. In vitro, Ro 15-4513 competitively inhibits ethanol binding to the GABAA receptor complex. In vivo, Ro 154513 inhibits the sedation caused by alcohol but does n ...
Cell Cycle Regulation in Rat 1 Fibroblasts Expressing a Murine
... useful tools in the study of receptor sequestration and trafficking. We have used this technique previously to study a GFP-tagged TRH receptor construct [I]. In this study we have linked various N-terminally Flag tagged beta-adrenergic receptors with GFP at the C-terminus, and stably transfected the ...
... useful tools in the study of receptor sequestration and trafficking. We have used this technique previously to study a GFP-tagged TRH receptor construct [I]. In this study we have linked various N-terminally Flag tagged beta-adrenergic receptors with GFP at the C-terminus, and stably transfected the ...
5HT1F- and 5HT7-Receptor Agonists for the Treatment of Migraines
... were no cardiovascular effects (assessed by blood pressure, pulse, or ECG). The compound had good oral bioavailability with a tmax, between 1 and 2 h and an elimination half-life of 15 h [42]. Subsequently, data from phase II studies have been published showing that oral doses of 60 and 200 mg of LY ...
... were no cardiovascular effects (assessed by blood pressure, pulse, or ECG). The compound had good oral bioavailability with a tmax, between 1 and 2 h and an elimination half-life of 15 h [42]. Subsequently, data from phase II studies have been published showing that oral doses of 60 and 200 mg of LY ...
Pharmacology
... responses to drugs caused by genetic differences between individuals. Responses that are not found in the general population, such as general toxic effects, allergies, or side effects, but due to an inherited trait that produces a diminished or enhanced response to a drug. • Differences in Enzyme Ac ...
... responses to drugs caused by genetic differences between individuals. Responses that are not found in the general population, such as general toxic effects, allergies, or side effects, but due to an inherited trait that produces a diminished or enhanced response to a drug. • Differences in Enzyme Ac ...
NTs
... • Synaptic vesicles made by Golgi apparatus in cell body • Precursors, enzymes, and vesicles are transported from cell body down axon to terminal • At terminal, NTs are synthesized and packaged into vesicles • Filled vesicles dock onto proteins in terminal ...
... • Synaptic vesicles made by Golgi apparatus in cell body • Precursors, enzymes, and vesicles are transported from cell body down axon to terminal • At terminal, NTs are synthesized and packaged into vesicles • Filled vesicles dock onto proteins in terminal ...
Introduction to neuropharmacology
... Pharmacology is the science that study the interaction of drugs with biological systems either in vivo, ex vivo or in vitro. Pharmacology comes from pharmakon, poison or drug in Greek. In Spanish there is a handy word farmaco that is lacking in English. Drug is defined as any natural or synthetic mo ...
... Pharmacology is the science that study the interaction of drugs with biological systems either in vivo, ex vivo or in vitro. Pharmacology comes from pharmakon, poison or drug in Greek. In Spanish there is a handy word farmaco that is lacking in English. Drug is defined as any natural or synthetic mo ...
Document
... histamine synthesis and release in the CNS”; one step up in the chain of histamine action H4: found primarily in intestinal tissue, spleen, thymus, and immune active cells (such as T cells, neutrophils, and eosinophils), “which suggests an important role for H4 receptors in the regulation of immune ...
... histamine synthesis and release in the CNS”; one step up in the chain of histamine action H4: found primarily in intestinal tissue, spleen, thymus, and immune active cells (such as T cells, neutrophils, and eosinophils), “which suggests an important role for H4 receptors in the regulation of immune ...
Drug-Receptor Interactions
... when the membrane is depolarized to a threshold potential and contribute to further membrane depolarization by allowing Na+ influx into the cell. Ligand-gated ion channels are activated after binding to specific ligands or drugs. Many neurotransmitters and drugs activate membrane- bound ligand ion - ...
... when the membrane is depolarized to a threshold potential and contribute to further membrane depolarization by allowing Na+ influx into the cell. Ligand-gated ion channels are activated after binding to specific ligands or drugs. Many neurotransmitters and drugs activate membrane- bound ligand ion - ...
5th Lecture 1433
... For constitutively active receptors, an appreciable proportion of receptors adopt the R* conformation in the absence of any ligand Agonists have higher affinity for R* than for R and thus shift the equilibrium from the resting state (R) to the active (R*) state and hence, produce a response ...
... For constitutively active receptors, an appreciable proportion of receptors adopt the R* conformation in the absence of any ligand Agonists have higher affinity for R* than for R and thus shift the equilibrium from the resting state (R) to the active (R*) state and hence, produce a response ...
Summary overview: Gi and Gs G-protein coupled receptors - Di-Et-Tri
... . An inhibitory Giα, when it binds GTP, inhibits Adenylate cyclase. Different effectors & their receptors induce Giα to exchange GDP for GTP than those that activate Gsα. In some cells, the complex of Gβγ that is released when Ga binds GTP is itself an effector that binds to and activates other prot ...
... . An inhibitory Giα, when it binds GTP, inhibits Adenylate cyclase. Different effectors & their receptors induce Giα to exchange GDP for GTP than those that activate Gsα. In some cells, the complex of Gβγ that is released when Ga binds GTP is itself an effector that binds to and activates other prot ...
351 Pharmacology 3rd sf
... Down-regulation “A decrease in the total number of target-cell receptors for a given messenger/ligand in response to chronic high extracellular concentration of the messenger/ligand” Up-regulation “An increase in the total number of target-cell receptors for a given messenger/ligand in response ...
... Down-regulation “A decrease in the total number of target-cell receptors for a given messenger/ligand in response to chronic high extracellular concentration of the messenger/ligand” Up-regulation “An increase in the total number of target-cell receptors for a given messenger/ligand in response ...