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VU-0152100
VU-0152100 is a positive modulator of the M4 receptor, one of the muscarinic acetylcholine receptors. Treatment of stimulant addiction In mice, VU-0152100 is able to decrease self-administration of cocaine, this is thought to come from the M4 receptor's action on D1 containing dopaminergic neurons. It is also able to almost completely inhibit the hyperactivity Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple ... caused by cocaine. Another study has shown that this drug is able to reverse hyperlocomotion induced by amphetamine, in an anti-psychotic-like manner. This data suggests that it could potentially be developed as a treatment for stimulant abuse. See also * VU-0152099 References M4 receptor positive allosteric modulators Thienopyridines Carboxamides 4-Methoxy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Acetylcholine Receptor M4
The muscarinic acetylcholine receptor M4, also known as the cholinergic receptor, muscarinic 4 (CHRM4), is a protein that, in humans, is encoded by the ''CHRM4'' gene. Function M4 muscarinic receptors are coupled to Gi/o heterotrimeric proteins. They function as inhibitory autoreceptors for acetylcholine. Activation of M4 receptors inhibits acetylcholine release in the striatum. The M2 subtype of acetylcholine receptor functions similarly as an inhibitory autoreceptor to acetylcholine release, albeit functioning actively primarily in the hippocampus and cerebral cortex. Muscarinic acetylcholine receptors possess a regulatory effect on dopaminergic neurotransmission. Activation of M4 receptors in the striatum inhibit D1-induced locomotor stimulation in mice. M4 receptor-deficient mice exhibit increased locomotor simulation in response to D1 agonists, amphetamine and cocaine. Neurotransmission in the striatum influences extrapyramidal motor control, thus alterations in M4 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
VU-0152099
VU-0152099 is a positive allosteric modulator of the M4 receptor used in scientific research. Mechanism of action VU-0152099 is a positive allosteric modulator acting at M4 receptors, it lacks agonist activity, which means it cannot activate the receptor on its own, but can potentiate the activity of M4 receptor agonists such as acetylcholine. Potential use In rats, VU-0152099 is able to decrease self-administration of cocaine and reverse hyperlocomotion induced by amphetamine. These tests show that VU-0152099 could potentially be developed as a treatment for addiction to stimulants. See also * VU-0152100 VU-0152100 is a positive modulator of the M4 receptor, one of the muscarinic acetylcholine receptors. Treatment of stimulant addiction In mice, VU-0152100 is able to decrease self-administration of cocaine, this is thought to come from the M4 ... References {{Muscarinic acetylcholine receptor modulators Amines Benzodioxoles Carboxamides M4 receptor posit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Acetylcholine Receptor
Muscarinic acetylcholine receptors (mAChRs) are acetylcholine receptors that form G protein-coupled receptor, G protein-coupled receptor complexes in the cell membranes of certain neurons and other Cell (biology), cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibers. They are mainly found in the parasympathetic nervous system, but also have a role in the sympathetic nervous system in the control of Sweat gland, sweat glands. Muscarinic receptors are so named because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpine and Hyoscine hydrobromide, scopolamine) manipulate these two distinct receptors by acting as selective agonists or receptor antagonist, antagonists. Function acetylcholine, Ac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Receptor D4
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 has been 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 11p15.5. Th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hyperlocomotion
Locomotor activity is a measure of animal behavior which is employed in scientific research. Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in which locomotor activity (locomotion) is increased. It is induced by certain drugs like psychostimulants and NMDA receptor antagonists and is reversed by certain other drugs like antipsychotics and certain antidepressants. Stimulation of locomotor activity is thought to be mediated by increased signaling in the nucleus accumbens, a major brain area involved in behavioral activation and motivated behavior. Hypolocomotion, also known as locomotor hypoactivity, hypoactivity, and decreased locomotor activity, is an effect of certain drugs in animals in which locomotor activity is decreased. It is a characteristic effect of many sedative agents and general anesthetics. Antipsychotics, which are dopamine receptor antagonists, and many serotonerg ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
M4 Receptor Positive Allosteric Modulators
M4 or M-4 most often refers to: * M4 carbine, an American carbine * M4 Sherman, an American World War II medium tank M4, M04, or M-4 may also refer to: Arts and entertainment * ''M4'' (EP), a 2006 EP by Faunts * ''M4'' (video game), a 1992 computer game developed for the Macintosh * ''M.IV'' ("Matrix IV"), the fictional Warner Brothers videogame project inside the 2021 film ''The Matrix Resurrections'' * Former name of band First to Eleven * M4, the robot assistant to the character Flint in the Star Trek episode Requiem for Methuselah Military Weapons * Benelli M4 Super 90, an Italian semi-automatic,gas-operated shotgun * M4 autocannon, an American 37 mm automatic gun * M4 Selectable Lightweight Attack Munition (SLAM), an American land mine * M4 SLBM, a French submarine-launched ballistic missile from 1985 * M4 Survival Rifle, an American rifle in aircraft survival gear * Spectre M4, an Italian submachine gun * M4 bayonet, an American World War II bayonet used f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thienopyridines
Thienopyridines are a class of selective, irreversible ADP receptor/P2Y12 inhibitors used for their anti-platelet activity. They have a significant role in the management of cardiovascular disease. Clinical Uses They are used in the management of peripheral artery disease, as well as the prevention of coronary stent thrombosis and strokes. Examples Drugs in this class include: clopidogrel (Plavix), prasugrel (Effient), and ticlopidine (Ticlid). Tinoridine was actually a predecessor to this work. Alternatives Ticagrelor Ticagrelor, sold under the brand name Brilinta among others, is a medication used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. I ... (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that is distinct from the mechanism of the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
