Depression and Suicide
... TRICYCLIC ANTIDEPRESSANTS As a group they are more “mixed” in monoamine activity than modern agents e.g. closer ratio of noradrenaline / serotonin activity than NARIs or SSRIs Main postulated action re-uptake inhibition, but have effects on 5HT1a, 5HT2 and NA ß receptors Relatively little effect on ...
... TRICYCLIC ANTIDEPRESSANTS As a group they are more “mixed” in monoamine activity than modern agents e.g. closer ratio of noradrenaline / serotonin activity than NARIs or SSRIs Main postulated action re-uptake inhibition, but have effects on 5HT1a, 5HT2 and NA ß receptors Relatively little effect on ...
No Slide Title
... • Activation of SXR may predict effects of suspected EDC – SXR activators may be detoxified by CYP action and not a human risk – But activators may also be toxified by CYP action, increasing the risk. – EDC may have no effect on SXR and therefore more likely to act on other receptors, e.g. ER ...
... • Activation of SXR may predict effects of suspected EDC – SXR activators may be detoxified by CYP action and not a human risk – But activators may also be toxified by CYP action, increasing the risk. – EDC may have no effect on SXR and therefore more likely to act on other receptors, e.g. ER ...
No Slide Title - Bruce Blumberg
... • Activation of SXR may predict effects of suspected EDC – SXR activators may be detoxified by CYP action and not a human risk – But activators may also be toxified by CYP action, increasing the risk. – EDC may have no effect on SXR and therefore more likely to act on other receptors, e.g. ER ...
... • Activation of SXR may predict effects of suspected EDC – SXR activators may be detoxified by CYP action and not a human risk – But activators may also be toxified by CYP action, increasing the risk. – EDC may have no effect on SXR and therefore more likely to act on other receptors, e.g. ER ...
Extracellular serotonin in the lateral hypothalamic area is increased
... Experiment 2a: effects of increasing 5-HT in the LHAA on copulatory behavior Microinjection of alaproclate (n 5 12) dose-dependently impaired copulatory performance. All of the subjects in the 0.0 mg condition copulated to ejaculation. In the 10.0 mg condition, only 10 subjects mounted, 9 intromitte ...
... Experiment 2a: effects of increasing 5-HT in the LHAA on copulatory behavior Microinjection of alaproclate (n 5 12) dose-dependently impaired copulatory performance. All of the subjects in the 0.0 mg condition copulated to ejaculation. In the 10.0 mg condition, only 10 subjects mounted, 9 intromitte ...
The receptors have a long extracellular domain
... • Neurotransmitter binding and ion flux are provided by two or more individual molecules. • Allows for many effects of NT on postsynaptic cell • Can regulate several channels, metabolic enzymes and gene expression • Stimulates or inhibits second messengers ...
... • Neurotransmitter binding and ion flux are provided by two or more individual molecules. • Allows for many effects of NT on postsynaptic cell • Can regulate several channels, metabolic enzymes and gene expression • Stimulates or inhibits second messengers ...
Autonomic Nervous System
... (metered dose inhaler) or by nebulizer mask driven by oxygen or air. Aerochamber is better To test how full an MDI container is -see figure ...
... (metered dose inhaler) or by nebulizer mask driven by oxygen or air. Aerochamber is better To test how full an MDI container is -see figure ...
3rd year antidepressant part 2a2011-09-11 10
... 5-HT1-receptors are predominantly inhibitory in their effects. 5-HT1A-receptors are expressed as autoreceptors by the 5-HT neurons in the raphe nuclei, and their autoinhibitory effect tends to limit the rate of firing of these cells. They are also widely distributed in the limbic system and are bel ...
... 5-HT1-receptors are predominantly inhibitory in their effects. 5-HT1A-receptors are expressed as autoreceptors by the 5-HT neurons in the raphe nuclei, and their autoinhibitory effect tends to limit the rate of firing of these cells. They are also widely distributed in the limbic system and are bel ...
2nd Lecture 1433
... The extent to which the ligand/drug is capable of binding and remained bound to receptor. High Affinity – the ligand binds well and remains bound long enough to activate the receptor. Low Affinity – the ligand binds less well and may not remain bound long enough to activate the receptor. ...
... The extent to which the ligand/drug is capable of binding and remained bound to receptor. High Affinity – the ligand binds well and remains bound long enough to activate the receptor. Low Affinity – the ligand binds less well and may not remain bound long enough to activate the receptor. ...
ppt
... G protein-coupled receptors • Receptors on the inner face of the plasma membrane regulate or facilitate effector proteins through a group of guanosine triphosphate (GTP) proteins known as G proteins. • Some hormones peptide receptors and neurotransmitter receptors (e.g., adrenergic and moscarinic ...
... G protein-coupled receptors • Receptors on the inner face of the plasma membrane regulate or facilitate effector proteins through a group of guanosine triphosphate (GTP) proteins known as G proteins. • Some hormones peptide receptors and neurotransmitter receptors (e.g., adrenergic and moscarinic ...
Drugs for Depressive Disorders
... release of norepinephrine from noradrenergic nerve endings, and of serotonin from serotonergic nerve endings. ➼ Blockade of 5-HT2A/C presynaptic receptors. ☛ (It is not known which one of those two actions is more important for the ...
... release of norepinephrine from noradrenergic nerve endings, and of serotonin from serotonergic nerve endings. ➼ Blockade of 5-HT2A/C presynaptic receptors. ☛ (It is not known which one of those two actions is more important for the ...
Chapter 17 Antipsychotic Agents
... Tricyclics antidepressants block the amine (norepinephrine or serotonin) reuptake pumps. Such an action presumably permits a longer sojourn逗留 of neurotransmitter at the receptor site. (The pathogenesis of depression- the Amine-Hypothesis) ...
... Tricyclics antidepressants block the amine (norepinephrine or serotonin) reuptake pumps. Such an action presumably permits a longer sojourn逗留 of neurotransmitter at the receptor site. (The pathogenesis of depression- the Amine-Hypothesis) ...
1B Ulcer Medicines
... in the stomach wall, but an enzyme (15-hydroxyprostaglandin dehydrogenase) stops the prostaglandins from working. Licorice blocks this enzyme, and so the prostaglandins stick around longer, make ulcers heal. HOWEVER chemistry always has a price, licorice causes cortisol to bind to a protein causing ...
... in the stomach wall, but an enzyme (15-hydroxyprostaglandin dehydrogenase) stops the prostaglandins from working. Licorice blocks this enzyme, and so the prostaglandins stick around longer, make ulcers heal. HOWEVER chemistry always has a price, licorice causes cortisol to bind to a protein causing ...
Review of Principles
... Some tissues have more receptors than are necessary to produce a maximal response. – Dependent on tissue, measure of response and intrinsic efficacy of the drug. ...
... Some tissues have more receptors than are necessary to produce a maximal response. – Dependent on tissue, measure of response and intrinsic efficacy of the drug. ...
Hallucinogens & Perception
... Gonzalez-Maeso J, Weisstaub NV, et al (2007) Hallucinogens Recruit Specific Cortical 5-HT(2A) Receptor- Mediated Signaling Pathways to Affect Behavior. Neuron 53: 439-52 Gouzoulis-Mayfrank E, Hermle L, Thelen B, Sass H (1998) History, rationale and potential of human experimental hallucinogenic drug ...
... Gonzalez-Maeso J, Weisstaub NV, et al (2007) Hallucinogens Recruit Specific Cortical 5-HT(2A) Receptor- Mediated Signaling Pathways to Affect Behavior. Neuron 53: 439-52 Gouzoulis-Mayfrank E, Hermle L, Thelen B, Sass H (1998) History, rationale and potential of human experimental hallucinogenic drug ...
Atypical Antipsychotic Drugs: Clozapine, olanzapine
... hydroxyrisperidone in vivo in most patients, except for about 10% of patients who are poor metabolizers. These drugs have complex pharmacology but they share a greater ability to alter 5-HT 2A -receptor activity than to interfere with D 2 -receptor action. In most cases, they act as partial agonist ...
... hydroxyrisperidone in vivo in most patients, except for about 10% of patients who are poor metabolizers. These drugs have complex pharmacology but they share a greater ability to alter 5-HT 2A -receptor activity than to interfere with D 2 -receptor action. In most cases, they act as partial agonist ...
Pharmacokinetics - The Cambridge MRCPsych Course
... the natural neurotransmitter May compete with a natural neurotransmitter for binding at receptor Example: first-generation antipsychotics ...
... the natural neurotransmitter May compete with a natural neurotransmitter for binding at receptor Example: first-generation antipsychotics ...
Review notes
... (Incoming signal from different receptor) Homologous desensitization (only occurs on receptor which has already been stimulated) Lipid soluble ligands that penetrate cell membrane, Receptors contain DNA-binding domains (transcriptional activators/suppressors) Takes longer to act—requires penetration ...
... (Incoming signal from different receptor) Homologous desensitization (only occurs on receptor which has already been stimulated) Lipid soluble ligands that penetrate cell membrane, Receptors contain DNA-binding domains (transcriptional activators/suppressors) Takes longer to act—requires penetration ...