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Corticotropin-releasing Hormone Antagonist
A Corticotropin-releasing hormone antagonist (CRH antagonist) is a specific type of receptor antagonist that blocks the receptor sites for corticotropin-releasing hormone, also known as corticotropin-releasing factor (CRF), which synchronizes the behavioral, endocrine, autonomic, and immune responses to stress by controlling the hypothalamic-pituitary-adrenal axis (HPA axis). CRH antagonists thereby block the consequent secretions of ACTH and cortisol due to stress, among other effects. CRH receptor subtypes There are four subtypes of the CRH receptor known at present, defined as CRF-1, CRF-2a, CRF-2b, and CRF-2g. Three of these receptors are expressed only in the brain: CRF-1 in the cortex and cerebrum, CRF-2a in the lateral septum and hypothalamus, and CRF-2g in the amygdala. CRF-2b is expressed in the choroid plexus and cerebral arterioles in the brain, but is expressed mainly peripherally on the heart and skeletal muscle tissue. Extensive research has shown that overactivity ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
Corticotropin-releasing Hormone
Corticotropin-releasing hormone (CRH) (also known as corticotropin-releasing factor (CRF) or corticoliberin; corticotropin may also be spelled corticotrophin) is a peptide hormone involved in stress (biology), stress responses. It is a releasing hormone that belongs to corticotropin-releasing factor family. In humans, it is encoded by the ''CRH'' gene. Its main function is the stimulation of the pituitary synthesis of adrenocorticotropic hormone (ACTH), as part of the hypothalamic–pituitary–adrenal axis (HPA axis). Corticotropin-releasing hormone (CRH) is a 41-amino acid peptide derived from a 196-amino acid preprohormone. CRH is secreted by the paraventricular nucleus (PVN) of the hypothalamus in response to stress (biological), stress. Increased CRH production has been observed to be associated with Alzheimer's disease and major depression, and autosomal recessive hypothalamic corticotropin deficiency has multiple and potentially fatal metabolic consequences including hypo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACTH
Adrenocorticotropic hormone (ACTH; also adrenocorticotropin, corticotropin) is a polypeptide tropic hormone produced by and secreted by the anterior pituitary gland. It is also used as a medication and diagnostic agent. ACTH is an important component of the hypothalamic-pituitary-adrenal axis and is often produced in response to biological stress (along with its precursor corticotropin-releasing hormone from the hypothalamus). Its principal effects are increased production and release of cortisol by the cortex of the adrenal gland. ACTH is also related to the circadian rhythm in many organisms. Deficiency of ACTH is an indicator of secondary adrenal insufficiency (suppressed production of ACTH due to an impairment of the pituitary gland or hypothalamus, cf. hypopituitarism) or tertiary adrenal insufficiency (disease of the hypothalamus, with a decrease in the release of corticotropin releasing hormone (CRH)). Conversely, chronically elevated ACTH levels occur in primary adren ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cortisol
Cortisol is a steroid hormone, in the glucocorticoid class of hormones. When used as a medication, it is known as hydrocortisone. It is produced in many animals, mainly by the ''zona fasciculata'' of the adrenal cortex in the adrenal gland. It is produced in other tissues in lower quantities. It is released with a diurnal cycle and its release is increased in response to stress and low blood-glucose concentration. It functions to increase blood sugar through gluconeogenesis, to suppress the immune system, and to aid in the metabolism of fat, protein, and carbohydrates. It also decreases bone formation. Many of these functions are carried out by cortisol binding to glucocorticoid or mineralocorticoid receptors inside the cell, which then bind to DNA to impact gene expression. Health effects Metabolic response Metabolism of glucose In general, cortisol stimulates gluconeogenesis (the synthesis of 'new' glucose from non-carbohydrate sources, which occurs mainly in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cerebrospinal Fluid
Cerebrospinal fluid (CSF) is a clear, colorless body fluid found within the tissue that surrounds the brain and spinal cord of all vertebrates. CSF is produced by specialised ependymal cells in the choroid plexus of the ventricles of the brain, and absorbed in the arachnoid granulations. There is about 125 mL of CSF at any one time, and about 500 mL is generated every day. CSF acts as a shock absorber, cushion or buffer, providing basic mechanical and immunological protection to the brain inside the skull. CSF also serves a vital function in the cerebral autoregulation of cerebral blood flow. CSF occupies the subarachnoid space (between the arachnoid mater and the pia mater) and the ventricular system around and inside the brain and spinal cord. It fills the ventricles of the brain, cisterns, and sulci, as well as the central canal of the spinal cord. There is also a connection from the subarachnoid space to the bony labyrinth of the inner ear via the perilymphat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antalarmin
Antalarmin (CP-156,181) is a drug that acts as a CRH1 antagonist. Corticotropin-releasing hormone (CRH), also known as Corticotropin-releasing factor, is an endogenous peptide hormone released in response to various triggers such as chronic stress and drug addiction. Such triggers result in the release of corticotropin (ACTH), another hormone involved in the physiological response to stress. Chronic release of CRH and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive glucocorticoid release, stomach ulcers, anxiety, diabetes mellitus, osteoporosis, depression, and development of high blood pressure and consequent cardiovascular problems. Antalarmin is a non-peptide drug that blocks the CRH1 receptor, and, as a consequence, reduces the release of ACTH in response to chronic stress. This has been demonstrated in animals to reduce the behavioral responses to stressful situations, and it is proposed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pexacerfont
Pexacerfont (INN, previously known as BMS-562,086) is a drug developed by Bristol-Myers Squibb which acts as a CRF1 antagonist. Corticotropin-releasing factor (CRF), also known as corticotropin-releasing hormone, is an endogenous peptide hormone which is released in response to various triggers such as chronic stress. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress. Chronic release of CRF and ACTH is believed to be directly or indirectly involved in many of the harmful physiological effects of chronic stress, such as excessive glucocorticoid release, diabetes mellitus, osteoporosis, stomach ulcers, anxiety, depression, and development of high blood pressure and consequent cardiovascular problems. Pexacerfont is a recently developed CRF-1 antagonist which was in clinical trials for the treatment of anxiety disorders, and has also been proposed to be useful for the treatment of depression and irrita ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
General Anxiety Disorder
Generalized anxiety disorder (GAD) is a mental and behavioral disorder, specifically an anxiety disorder characterized by excessive, uncontrollable and often irrational worry about events or activities. Worry often interferes with daily functioning, and individuals with GAD are often overly concerned about everyday matters such as health, finances, death, family, relationship concerns, or work difficulties."What Is Generalized Anxiety Disorder?" National Institute of Mental Health. Accessed 28 May 2008. Symptoms may include excessive worry, restlessness, , exhaustion, irritability, sweating, and |
CP-154,526
CP-154,526 is a potent and selective antagonist of the corticotropin releasing hormone receptor 1 developed by Pfizer. CP-154,526 is under investigation for the potential treatment of alcoholism. See also * Antalarmin * Pexacerfont * Corticotropin releasing hormone antagonist A Corticotropin-releasing hormone antagonist (CRH antagonist) is a specific type of receptor antagonist that blocks the receptor sites for corticotropin-releasing hormone, also known as corticotropin-releasing factor (CRF), which synchronizes the be ... References Further reading * * * External links * Anxiolytics Corticotropin-releasing hormone antagonists Pyrrolopyrimidines Pfizer brands {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Astressin-B
Astressin-B is a nonselective corticotropin releasing hormone antagonist that reduces the synthesis of adrenocorticotropic hormone and cortisol. It reduces the synthesis of adrenocorticotropic hormone and improves the sexual drive of rats under stressing conditions. Astressin-B is able to delay the emptying of solid food in mice. Astressin-B can prevent the release of adrenocorticotropic hormone in mice due to shock, alcohol and endotoxemia. Treatment with astressin-B caused the sudden growth of hair in mice bred for a propensity for stress Stress may refer to: Science and medicine * Stress (biology), an organism's response to a stressor such as an environmental condition * Stress (linguistics), relative emphasis or prominence given to a syllable in a word, or to a word in a phrase .... References Corticotropin-releasing hormone Corticotropin-releasing hormone antagonists {{biochem-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SSRI
Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs increase the extracellular level of the neurotransmitter serotonin by limiting its reabsorption (reuptake) into the presynaptic cell. They have varying degrees of selectivity for the other monoamine transporters, with pure SSRIs having strong affinity for the serotonin transporter and only weak affinity for the norepinephrine and dopamine transporters. SSRIs are the most widely prescribed antidepressants in many countries. The efficacy of SSRIs in mild or moderate cases of depression has been disputed and may or may not be outweighed by side effects, especially in adolescent populations. Medical uses The main indication for SSRIs is major depressive disorder; however, they are frequently prescribed for anxiety disorders, such as social anxiety disorder, general ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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