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BIBP-3226
BIBP-3226 is a drug used in scientific research which acts as a potent and selective antagonist for both the Neuropeptide Y receptor Y1 and also the neuropeptide FF receptor. It was the first non-peptide antagonist developed for the Y1 receptor and has been widely used to help determine its functions in the body. Activation of Y1 is thought to be involved in functions such as regulation of appetite and anxiety, and BIBP-3226 has anxiogenic and anorectic effects, as well as blocking the Y1-mediated corticotropin releasing hormone release. It has also been used as a lead compound A lead compound (, i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but ... to develop a number of newer more potent Y1 antagonists. References Neuropeptide Y antagonists {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide Y Receptor Y1
Neuropeptide Y receptor type 1 is a protein that in humans is encoded by the ''NPY1R'' gene. Selective ligands Agonists * Neuropeptide Y (endogenous agonist, non subtype selective) * Peptide YY Antagonists ;Peptide * BVD-10 (selective NPY1 antagonist, CAS# 262418-00-8) * GR-231,118 (mixed NPY1 antagonist / NPY4 agonist, CAS# 158859-98-4) ;Non-peptide * BIBO-3304 (CAS# 191868-14-1) * BIBP-3226 (CAS# 159013-54-4) * PD-160,170 (CAS# 181468-88-2) Available Structures 5ZBH(Neuropeptide Y1 bound to antagonist BMS-193835) 5ZBQ(Neuropeptide Y1 bound to antagonist UR-MK299) See also * Neuropeptide Y receptor Neuropeptide Y receptors are a family of receptors belonging to class A G-protein coupled receptors and they are activated by the closely related peptide hormones neuropeptide Y, peptide YY and pancreatic polypeptide. These receptors are invo ... References Further reading * * * * * * * * * * * * * * External links * * G protein-cou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuropeptide FF Receptor
The neuropeptide FF receptors are members of the G-protein coupled receptor superfamily of integral membrane proteins which bind the pain modulatory neuropeptides AF and FF. The Neuropeptide FF receptor family is a member of the G protein-coupled receptor superfamily containing two subtypes, NPFF1 and NPFF2, which exhibit a high affinity for Neuropeptide FF (NPFF) peptides. NPFF1 is broadly distributed in the central nervous system with the highest levels found in the limbic system and the hypothalamus. NPFF2 is present in high density, particularly in mammals in the superficial layers of the spinal cord where it is involved in nociception and modulation of opioid functions. These receptors participate to the modulation of opioid receptor function in the brain and spinal cord, and can either reduce or increase opioid receptor function depending which tissue they are released in, reflecting a complex role for neuropeptide FF in pain responses. NPFF receptors are coupled to G prote ... [...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, |
Neuropeptide Y
Neuropeptide Y (NPY) is a 36 amino-acid neuropeptide that is involved in various physiological and homeostatic processes in both the central and peripheral nervous systems. NPY has been identified as the most abundant peptide present in the mammalian central nervous system, which consists of the brain and spinal cord. It is secreted alongside other neurotransmitters such as GABA and glutamate. In the autonomic system it is produced mainly by neurons of the sympathetic nervous system and serves as a strong vasoconstrictor and also causes growth of fat tissue. In the brain, it is produced in various locations including the hypothalamus, and is thought to have several functions, including: increasing food intake and storage of energy as fat, reducing anxiety and stress, reducing pain perception, affecting the circadian rhythm, reducing voluntary alcohol intake, lowering blood pressure, and controlling epileptic seizures. Function Neuropeptide Y has been identified as be ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
British Journal Of Pharmacology
The ''British Journal of Pharmacology'' is a biweekly peer-reviewed medical journal covering all aspects of experimental pharmacology. It is published for the British Pharmacological Society by Wiley-Blackwell. It was established in 1946 as the ''British Journal of Pharmacology and Chemotherapy''. The journal obtained its current title in 1968. The current editor-in-chief is Amrita Ahluwalia. Previous editors-in-chief include Ian McGrath, Humphrey Rang, Alan North, Phil Moore, Bill Large, and Tony Birmingham. A sister journal, also published for the British Pharmacological Society by Wiley-Blackwell is the ''British Journal of Clinical Pharmacology''. The journal publishes research papers, review articles, commentaries and correspondence in all fields of pharmacology. It also publishes themed issues, as well as supplements. ''The Concise Guide to PHARMACOLOGY'' The ''Concise Guide to PHARMACOLOGY'' is a supplement of the ''British Journal of Pharmacology'', replacing the "Guid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anxiogenic
An anxiogenic or panicogenic substance is one that causes anxiety. This effect is in contrast to anxiolytic agents, which inhibits anxiety. Together these categories of psychoactive compounds may be referred to as anxiotropic compounds. Anxiogenic effects can be measured by, for example, the hole-board test in rats and mice. A number of agents are used to provoke anxiety (anxiogens) or panic (panicogens) in experimental models. Some of the most common substances are: carbon dioxide (as carbogen), sodium lactate, cocaine, substituted amphetamines, caffeine, L-DOPA, methylphenidate, modafinil, GABA antagonists such as DMCM, FG-7142 and ZK-93426, serotonergic agents such as mCPP and LY-293,284, adrenergic agents such as yohimbine, psychoactive agents such as THC and LSD in susceptible individuals, antipsychotics/ dopamine antagonists such as ecopipam and reserpine, and cholecystokinin (CCK) (especially the tetrapeptide and octapeptide fragments CCK-4 and CCK-8). Sodium ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anorectic
An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek ''ἀν-'' (an-) = "without" and ''ὄρεξις'' (órexis) = "appetite"), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term basis clinically to treat obesity, some appetite suppressants are also available over-the-counter. Most common natural appetite suppressants are based on '' Hoodia'', a genus of 13 species in the flowering plant family Apocynaceae, under the subfamily Asclepiadoideae. Several appetite suppressants are based on a mix of natural ingredients, mostly using green tea as its basis, in combination with other plant extracts such as fucoxanthin, found naturally in seaweed. Drugs of this class are frequently stimulants of the phenethylamine family, related to amphetamine. The German and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 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. 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 hypoglycemia. In addition to being pr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lead Compound
A lead compound (, i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by back-up compounds. Its chemical structure serves as a starting point for chemical modifications in order to improve potency, selectivity, or pharmacokinetic parameters. Furthermore, newly invented pharmacologically active moieties may have poor druglikeness and may require chemical modification to become drug-like enough to be tested biologically or clinically. Terminology Lead compounds are sometimes called developmental candidates. This is because the discovery and selection of lead compounds occurs prior to preclinical and clinical development of the candidate. Discovering lead compo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
