WAY-100635
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WAY-100635
WAY-100635 is a piperazine drug and research chemical widely used in scientific studies. It was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor. It is sometimes referred to as a silent antagonist at the former receptor. It is closely related to WAY-100135. In light of its only recently discovered dopaminergic activity, conclusions drawn from studies that employed WAY-100635 as a selective 5-HT1A antagonist may need to be re-evaluated. Human PET studies In human PET studies WAY-100635 shows high binding in the cerebral cortex, hippocampus, raphe nucleus and amygdaloid nucleus, while lower in thalamus and basal ganglia. One study described a single case with relatively high binding in the cerebellum. In relating its binding to subject variables one Swedish study found WAY-100635 binding in raphe brain region correlating with self-transcendence and spiritual accep ...
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WAY-100135
WAY-100135 is a serotonergic drug of the phenylpiperazine family which is used in scientific research. It acts as potency (pharmacology), potent 5-HT1A receptor, 5-HT1A receptor receptor antagonist, antagonist, and was originally believed to be highly binding selectivity, selective, but further studies have demonstrated that it also acts as a partial agonist of the 5-HT1D, 5-HT1D receptor (pKi = 7.58; virtually the same affinity for 5-HT1A), and to a much lesser extent, of the 5-HT1B, 5-HT1B receptor (pKi = 5.82). These findings may have prompted the development of the related compound WAY-100635, another purportedly selective and even more potent 5-HT1A antagonist, which was synthesized shortly thereafter. However, WAY-100635 turned out to be non-selective as well, having been shown to act additionally as a potent D4 receptor, D4 receptor agonist later on. See also * WAY-100635 References

5-HT1A antagonists Carboxamides N-(2-methoxyphenyl)piperazines Tert-butyl comp ...
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5-HT1A
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor, or 5-HT receptor, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarisation and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neuromodulation 5-HT1A receptor ag ...
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D4 Receptor
The dopamine receptor D4 is a dopamine D2-like G protein-coupled receptor encoded by the gene on chromosome 11 at 11p15.5. The structure of DRD4 was recently reported in complex with the antipsychotic drug nemonapride. As with other dopamine receptor subtypes, the D4 receptor is activated by the neurotransmitter dopamine. It is linked to many neurological and psychiatric conditions including schizophrenia and bipolar disorder, ADHD, addictive behaviors, Parkinson's disease, and eating disorders such as anorexia nervosa. A weak association has been drawn between DRD4 and borderline personality disorder. It is also a target for drugs which treat schizophrenia and Parkinson's disease. The D4 receptor is considered to be D2-like in which the activated receptor inhibits the enzyme adenylate cyclase, thereby reducing the intracellular concentration of the second messenger cyclic AMP. Genetics The human protein is coded by the ''DRD4'' on chromosome 11 located in 11p15. ...
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Piperazine
Piperazine () is an organic compound that consists of a six-membered ring containing two nitrogen atoms at opposite positions in the ring. Piperazine exists as small alkaline deliquescent crystals with a saline taste. The piperazines are a broad class of chemical compounds, many with important pharmacological properties, which contain a core piperazine functional group. Origin and naming Piperazines were originally named because of their chemical similarity with piperidine, part of the structure of piperine in the black pepper plant (''Piper nigrum''). The -az- infix added to "piperazine" refers to the extra nitrogen atom, compared to piperidine. It is important to note, however, that piperazines are ''not'' derived from plants in the '' Piper'' genus. Chemistry Piperazine is freely soluble in water and ethylene glycol, but insoluble in diethyl ether. It is a weak base with two pKb of 5.35 and 9.73 at 25 °C.; the pH of a 10% aqueous solution of piperazine is 10.8–11.8. Pi ...
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Personality Trait
In psychology, trait theory (also called dispositional theory) is an approach to the study of human personality. Trait theorists are primarily interested in the measurement of ''traits'', which can be defined as habitual patterns of behaviour, thought, and emotion. According to this perspective, traits are aspects of personality that are relatively stable over time, differ across individuals (e.g. some people are outgoing whereas others are not), are relatively consistent over situations, and influence behaviour. Traits are in contrast to states, which are more transitory dispositions. In some theories and systems, traits are something a person either has or does not have, but in many others traits are dimensions such as extraversion vs. introversion, with each person rating somewhere along this spectrum. There are two approaches to define traits: as internal causal properties or as purely descriptive summaries. The internal causal definition states that traits influence our behav ...
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Journal Of Nuclear Medicine
''The Journal of Nuclear Medicine'' is a monthly peer-reviewed medical journal published by Society of Nuclear Medicine and Molecular Imaging that covers research on all aspects of nuclear medicine, including molecular imaging. Abstracting and indexing The journal is abstracted and indexed in Science Citation Index, Current Contents/Clinical Medicine, Current Contents/Life Sciences, BIOSIS Previews, and MEDLINE/PubMed. According to the ''Journal Citation Reports'', the journal has a 2020 impact factor The impact factor (IF) or journal impact factor (JIF) of an academic journal is a scientometric index calculated by Clarivate that reflects the yearly mean number of citations of articles published in the last two years in a given journal, as i ... of 10.057, ranking it 3rd out of 134 journals in the category "Radiology, Nuclear Medicine & Medical Imaging". References External links * {{DEFAULTSORT:Journal of Nuclear Medicine, The Radiology and medical imaging journals ...
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Journal Of Cerebral Blood Flow And Metabolism
The ''Journal of Cerebral Blood Flow & Metabolism'' is a monthly peer-reviewed medical journal the official journal of the International Society for Cerebral Blood Flow & Metabolism and publishes Peer review, peer-reviewed research and review papers. covering research on experimental, theoretical, and clinical aspects of brain circulation, metabolism and imaging. The editor-in-chief is Jun Chen (University of Pittsburgh). According to the ''Journal Citation Reports'', the journal has a 2020 impact factor of 6.200. References External links * International Society for Cerebral Blood Flow & Metabolism
Neuroscience journals Publications established in 1981 Nature Research academic journals English-language journals Monthly journals Delayed open access journals Academic journals associated with learned and professional societies {{neuroscience-journal-stub ...
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Raphe
Raphe (; from Greek ῥαφή, "seam"Liddell, H.G. & Scott, R. (1940). ''A Greek-English Lexicon. revised and augmented throughout by Sir Henry Stuart Jones. with the assistance of. Roderick McKenzie.'' Oxford: Clarendon Press.) has several different meanings in science. In botany and planktology it is commonly used when describing a seam or ridge on diatoms or seeds. In animal anatomy it is used to describe a ridged union of continuous biological tissue. There are several different significant anatomical raphes: * The raphe nucleus is a moderate-size cluster of nuclei found in the brain stem that releases serotonin to the rest of the brain. Selective serotonin reuptake inhibitor (SSRI) antidepressants are believed to act at these nuclei. * The buccal raphe, which is on the cheek and evidence of the fusion of the maxillary and mandibular processes * The lingual raphe on the tongue. Obvious physical evidence of the lingual raphe includes the frenulum (also called the frenum), ...
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Self-transcendence
Self-transcendence is a personality trait that involves the expansion of personal boundaries, including, potentially, experiencing spiritual ideas such as considering oneself an integral part of the universe. Several psychologists, including Viktor Frankl, Abraham Maslow, Pamela G. Reed, C. Robert Cloninger, Lars Tornstam, and Scott Barry Kaufman have made contributions to the theory of self-transcendence. Self-transcendence is distinctive as the first trait concept of a spiritual nature to be incorporated into a major theory of personality. Self-transcendence is one of the "character" dimensions of personality assessed in Cloninger's Temperament and Character Inventory. It is also assessed by the Self-Transcendence Scale and the Adult Self-Transcendence Inventory. Nature of the trait Several overlapping definitions of self-transcendence have been given. Viktor Frankl wrote, "The essentially self-transcendent quality of human existence renders man ''a being reaching out beyond ...
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Clinical Depression
Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Introduced by a group of US clinicians in the mid-1970s, the term was adopted by the American Psychiatric Association for this symptom cluster under mood disorders in the 1980 version of the ''Diagnostic and Statistical Manual of Mental Disorders'' (DSM-III), and has become widely used since. The diagnosis of major depressive disorder is based on the person's reported experiences, behavior reported by relatives or friends, and a mental status examination. There is no laboratory test for the disorder, but testing may be done to rule out physical conditions that can cause similar symptoms. The most common time of onset is in a person's 20s, with females affected about twice as often as males. The course of the disorder varies widely, from one epis ...
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American Journal Of Psychiatry
''The American Journal of Psychiatry'' is a monthly peer-reviewed medical journal covering all aspects of psychiatry, and is the official journal of the American Psychiatric Association. The first volume was issued in 1844, at which time it was known as the ''American Journal of Insanity''. The title changed to the current form with the July issue of 1921. According to the ''Journal Citation Reports'', the journal has a 2020 impact factor of 18.112. Ethical concerns Several complaints, including legal cases, have charged ''The American Journal of Psychiatry'' with being complicit in pharmaceutical industry corruption of clinical trial results. In a Department of Justice case against Forest Pharmaceuticals, Forest pleaded guilty to the charges of misbranding the drug Celexa (citalopram). The Complaint in Intervention clearly identifies a 2004 ghostwritten article published in ‘’The American Journal of Psychiatry'' in the names of Wagner ''et al.'' as a part of this illegal ma ...
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Thalamus
The thalamus (from Greek θάλαμος, "chamber") is a large mass of gray matter located in the dorsal part of the diencephalon (a division of the forebrain). Nerve fibers project out of the thalamus to the cerebral cortex in all directions, allowing hub-like exchanges of information. It has several functions, such as the relaying of sensory signals, including motor signals to the cerebral cortex and the regulation of consciousness, sleep, and alertness. Anatomically, it is a paramedian symmetrical structure of two halves (left and right), within the vertebrate brain, situated between the cerebral cortex and the midbrain. It forms during embryonic development as the main product of the diencephalon, as first recognized by the Swiss embryologist and anatomist Wilhelm His Sr. in 1893. Anatomy The thalamus is a paired structure of gray matter located in the forebrain which is superior to the midbrain, near the center of the brain, with nerve fibers projecting out to the ...
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