|
Ritanserin
Ritanserin, also known by its developmental code name R-55667, is a serotonin antagonist medication described as an anxiolytic, antidepressant, antiparkinsonian agent, and antihypertensive agent. It was never marketed for medical use due to safety problems but has been used in scientific research to study the serotonin system. Pharmacology Pharmacodynamics Ritanserin acts as a selective 5-HT2A (Ki = 0.45 nM) and 5-HT2C receptor (Ki = 0.71 nM) antagonist. It has relatively low affinity for the H1, D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). The affinity of ritanserin for the 5-HT1A receptor is less than 1 μM. In addition to its affinity for the 5-HT2A and 5-HT2C receptors, ritanserin also binds to and antagonizes the 5-HT1D, 5-HT2B, 5-HT5A, 5-HT6, and 5-HT7 receptors. History The atypical antipsychotic risperidone was developed from ritanserin. Society and culture Names ''Ritanserin'' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ritanserin Synthesis
Ritanserin, also known by its developmental code name R-55667, is a serotonin receptor antagonist, serotonin antagonist medication described as an anxiolytic, antidepressant, antiparkinsonian agent, and antihypertensive agent. It was never marketed for medical use due to drug safety, safety problems but has been used in scientific research to study the serotonin system. Pharmacology Pharmacodynamics Ritanserin acts as a selective 5-HT2A receptor, 5-HT2A (Ki = 0.45 nM) and 5-HT2C receptor, 5-HT2C receptor (Ki = 0.71 nM) receptor antagonist, antagonist. It has relatively low affinity (pharmacology), affinity for the Histamine H1 receptor, H1, D2 receptor, D2, alpha-1 adrenergic receptor, α1-adrenergic, and alpha-2 adrenergic receptor, α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively). The affinity of ritanserin for the 5-HT1A receptor, 5-HT1A receptor is less than 1 μM. In addition to its affinity for the 5-HT2A and 5-HT2C receptors, r ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Receptor Antagonist
A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors. Types 5-HT2A antagonists Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include, but are not limited to: * Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. * Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis. * Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors. 5-HT2A/2C antagonists * Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C and Alpha 1 (A1) adrenoreceptors. * Risperidone antipsychotic * Trazodone 5-HT3 antagonists Another subclass consists of drugs selectively acting at the 5-HT3 receptors, and thus are known as 5-HT3 antagonists. They are efficacious i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2C Receptor
The 5-HT2C receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gq/G11 and mediates excitatory neurotransmission. ''HTR2C'' denotes the human gene encoding for the receptor, that in humans is located at the X chromosome. As males have one copy of the gene and in females one of the two copies of the gene is repressed, polymorphisms at this receptor can affect the two sexes to differing extent. Structure At the cell surface the receptor exists as a homodimer. The crystal structure is known since 2018. Distribution 5-HT2C receptors are located mainly in the choroid plexus, and in rats is also found in many other brain regions in high concentrations, including parts of the hippocampus, anterior olfactory nucleus, substantia nigra, several brainstem nuclei, amygdala, subthalamic nucleus and lateral habenula. 5-HT2C receptors are also found on epithel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT7 Receptor
The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) The 5-HT7 receptor is coupled to Gs (stimulates the production of the intracellular signaling molecule cAMP) and is expressed in a variety of human tissues, particularly in the brain, the gastrointestinal tract, and in various blood vessels. This receptor has been a drug development target for the treatment of several clinical disorders. The 5-HT7 receptor is encoded by the ''HTR7'' gene, which in humans is transcribed into 3 different splice variants. Function When the 5-HT7 receptor is activated by serotonin, it sets off a cascade of events starting with release of the stimulatory G protein Gs from the GPCR complex. Gs in turn activates adenylate cyclase which increases intracellular levels of the second messenger cAMP. The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature and in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sleep
Sleep is a sedentary state of mind and body. It is characterized by altered consciousness, relatively inhibited sensory activity, reduced muscle activity and reduced interactions with surroundings. It is distinguished from wakefulness by a decreased ability to react to stimuli, but more reactive than a coma or disorders of consciousness, with sleep displaying different, active brain patterns. Sleep occurs in repeating periods, in which the body alternates between two distinct modes: REM sleep and non-REM sleep. Although REM stands for "rapid eye movement", this mode of sleep has many other aspects, including virtual paralysis of the body. Dreams are a succession of images, ideas, emotions, and sensations that usually occur involuntarily in the mind during certain stages of sleep. During sleep, most of the body's systems are in an anabolic state, helping to restore the immune, nervous, skeletal, and muscular systems; these are vital processes that maintain mood, memory, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Migraine
Migraine (, ) is a common neurological disorder characterized by recurrent headaches. Typically, the associated headache affects one side of the head, is pulsating in nature, may be moderate to severe in intensity, and could last from a few hours to three days. Non-headache symptoms may include nausea, vomiting, and photophobia, sensitivity to light, hyperacusis, sound, or Osmophobia, smell. The pain is generally made worse by physical activity during an attack,as PDF although regular physical exercise may prevent future attacks. Up to one-third of people affected have Aura (symptom), aura: typically, it is a short period of visual disturbance that signals that the headache will soon occur. Occasionally, aura can occur with little or no headache follow ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social withdrawal, decreased emotional expression, and apathy. Symptoms typically develop gradually, begin during young adulthood, and in many cases never become resolved. There is no objective diagnostic test; diagnosis is based on observed behavior, a history that includes the person's reported experiences, and reports of others familiar with the person. To be diagnosed with schizophrenia, symptoms and functional impairment need to be present for six months (DSM-5) or one month (ICD-11). Many people with schizophrenia have other mental disorders, especially substance use disorders, depressive disorders, anxiety disorders, and obsessive–compulsive disorder. About 0.3% to 0.7% of people are diagnosed with schizophrenia during their lifetime. In 2 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiety
Anxiety is an emotion which is characterized by an unpleasant state of inner turmoil and includes feelings of dread over anticipated events. Anxiety is different than fear in that the former is defined as the anticipation of a future threat whereas the latter is defined as the emotional response to a real threat. It is often accompanied by nervous behavior such as pacing back and forth, somatic complaints, and rumination. Anxiety is a feeling of uneasiness and worry, usually generalized and unfocused as an overreaction to a situation that is only subjectively seen as menacing. It is often accompanied by muscular tension, restlessness, fatigue, inability to catch one's breath, tightness in the abdominal region, nausea, and problems in concentration. Anxiety is closely related to fear, which is a response to a real or perceived immediate threat (fight or flight response); anxiety involves the expectation of future threat including dread. People facing anxiety may withdraw fro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Depression (mood)
Depression is a mental state of low mood and aversion to activity, which affects more than 280 million people of all ages (about 3.5% of the global population). Classified medically as a mental and behavioral disorder, the experience of depression affects a person's thoughts, behavior, motivation, feelings, and sense of well-being. The core symptom of depression is said to be anhedonia, which refers to loss of interest or a loss of feeling of pleasure in certain activities that usually bring joy to people. Depressed mood is a symptom of some mood disorders such as major depressive disorder and dysthymia; it is a normal temporary reaction to life events, such as the loss of a loved one; and it is also a symptom of some physical diseases and a side effect of some drugs and medical treatments. It may feature sadness, difficulty in thinking and concentration and a significant increase or decrease in appetite and time spent sleeping. People experiencing depression may have ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Generic Term
Trademark distinctiveness is an important concept in the law governing trademarks and service marks. A trademark may be eligible for registration, or registrable, if it performs the essential trademark function, and has distinctive character. Registrability can be understood as a continuum, with "inherently distinctive" marks at one end, "generic" and "descriptive" marks with no distinctive character at the other end, and "suggestive" and "arbitrary" marks lying between these two points. "Descriptive" marks must acquire distinctiveness through secondary meaning—consumers have come to recognize the mark as a source indicator—to be protectable. "Generic" terms are used to refer to the product or service itself and cannot be used as trademarks. The spectrum of distinctiveness In United States trademark law, Abercrombie & Fitch Co. v. Hunting World 537 F.2d 4 (2nd Cir. 1976) established the spectrum of trademark distinctiveness in the US, breaking trademarks into classes which ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It is taken either by mouth or by injection (subcutaneous or intramuscular). The injectable versions are long-acting and last for 2–4 weeks. Common side effects include extrapyramidal symptoms, movement problems, sedation, sleepiness, dizziness, trouble seeing, constipation, and increased weight. Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and hyperglycemia, high blood sugar levels. In older people with psychosis as a result of dementia, it may increase the risk of death. It is unknown if it is safe for use in pregnancy. Its mechanism of action is not entirely clear, but is believed to be related to its action as a dopamine antagonist, dopamine and serotonin antagonist. Study of risperidone began in the late 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
_1.jpg "Click for more on -> Migraine")
.svg "Click for more on -> Generic Term"){kind=logo}
