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CHF-1024
CHF-1024, also known as 5,6-dihydroxy-2-methylaminotetralin, is a dopamine D2 receptor agonist and α2-adrenergic receptor agonist of the 2-aminotetralin family. It is a cyclized phenethylamine analogue of the neurotransmitter dopamine. The drug is the active form of nolomirole (CHF-1035), a prodrug of CHF-1024 and the ''N'',''N''-diisobutyryl diester of the compound. Nolomirole was investigated for the treatment of heart failure but was never marketed. See also * Chiesi Farmaceutici * Nolomirole * Cyclized phenethylamine * Rotigotine * 5-OH-DPAT * 7-OH-DPAT 7-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with reasonable selectivity for the D3 receptor subtype, and low affinity for serotonin receptors, unlike its structural isomer 8-OH-DPAT. 7-OH-DPAT is self-administer ... * Carmoxirole References 2-Aminotetralins Alpha-2 adrenergic receptor agonists Catecholamines D2 receptor agonists Human drug metabolites {{Cardiovascul ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nolomirole
Nolomirole (; developmental code name CHF-1035), also known as 5,6-diisobutyryloxy-''N''-methyl-2-aminotetralin, is a dual dopamine D2 and α2-adrenergic receptor agonist which was under development for the treatment of heart failure but was never marketed. It is taken orally. Pharmacology The drug acts as an agonist of the dopamine D2 receptor, with an affinity (Ki) of 120nM for the (–)- enantiomer and 2,400nM for the (+)- enantiomer, and as an agonist of the α2-adrenergic receptor, with an affinity (Ki) of 130nM for the (–)- enantiomer and 1,600nM for the (+)- enantiomer. It is a prodrug of CHF-1024 (5,6-dihydroxy-''N''-methyl-2-aminotetralin), to which it is rapidly hydrolyzed by circulating esterase enzymes. The elimination half-life of nolomirole is said to be 3hours and its log P is 1.97. Chemistry Nolomirole and its active form CHF-1024 are cyclized phenethylamines and 2-aminotetralin analogues of the catecholamine neurotransmitter dopamine and its ''N''-m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2-aminotetralin
2-Aminotetralin (2-AT), also known as 1,2,3,4-tetrahydronaphthalen-2-amine (THN), is a stimulant drug with a chemical structure consisting of a tetralin core with an amine as substituent. 2-AT is a rigid analogue of phenylisobutylamine and fully substitutes for d-amphetamine in rat drug discrimination tests, although at one-half to one-eighth the potency. It showed greater potency than a variety of other amphetamine homologues, including 2-amino-1,2-dihydronapthalene (2-ADN), 2-aminoindane (2-AI), 1-naphthylaminopropane (1-NAP), 2-naphthylaminopropane (2-NAP), 1-phenylpiperazine (1-PP), , and . 2-AT has been shown to inhibit the reuptake of serotonin and norepinephrine, and might induce their release as well. It is also likely to act on dopamine on account of its full substitution of d-amphetamine in rodent studies. Chemical derivatives A number of derivatives of 2-aminotetralin exist, including: See also * 1-Aminotetralin 1-Aminotetralin (1-AT), also known as ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine
Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic chemical of the catecholamine and phenethylamine families. It is an amine synthesized by removing a carboxyl group from a molecule of its precursor chemical, L-DOPA, which is synthesized in the brain and kidneys. Dopamine is also synthesized in plants and most animals. In the brain, dopamine functions as a neurotransmitter—a chemical released by neurons (nerve cells) to send signals to other nerve cells. The brain includes several distinct dopamine pathways, one of which plays a major role in the motivational component of reward-motivated behavior. The anticipation of most types of rewards increases the level of dopamine in the brain, and many addictive drugs increase dopamine release or block its reuptake into neurons following release. Other brain dopamine pathways are involved in motor control and in controllin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chiesi Farmaceutici
Chiesi Farmaceutici S.p.A. is an Italian family controlled global pharmaceutical company based in Parma, Emilia-Romagna. Chiesi has 31 affiliates in the world, nearly 6,500 total employees and provides medicines to patients in 100 nations. Chiesi currently has revenues of 3 billion euros. According to 2020 official data from the European Patent Office (EPO), Chiesi Group, with 42 patents filed, is confirmed as the first Italian Pharmaceutical Company and third among Italian Companies across all sectors for filing the highest number of patents. In June 2019, Chiesi became a certified B Corporation, thus choosing to adopt a new legal status under US and Italian law. This ensures Chiesi legal protection to pursue a business model placing social and environmental values on equal footing with profits. Following the acquisition, in 1999, of Huddersfield based Trinity Pharmaceuticals, Chiesi has also had a significant presence in Manchester, United Kingdom. History Established in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catecholamines
A catecholamine (; abbreviated CA), most typically a 3,4-dihydroxyphenethylamine, is a monoamine neurotransmitter, an organic compound that has a catechol (benzene with two hydroxyl side groups next to each other) and a side-chain amine. Catechol can be either a free molecule or a substituent of a larger molecule, where it represents a 1,2-dihydroxybenzene group. Catecholamines are derived from the amino acid tyrosine, which is derived from dietary sources as well as synthesis from phenylalanine. Catecholamines are water-soluble and are 50% bound to plasma proteins in circulation. Included among catecholamines are epinephrine (adrenaline), norepinephrine (noradrenaline), and dopamine. Release of the hormones epinephrine and norepinephrine from the adrenal medulla of the adrenal glands is part of the fight-or-flight response. Tyrosine is created from phenylalanine by hydroxylation by the enzyme phenylalanine hydroxylase. Tyrosine is also ingested directly from dietar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-2 Adrenergic Receptor Agonists
Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor has two subclasses α1 and α2. Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity. The activation of α1 stimulates the membrane bound enzyme phospholipase C, and activation of α2 inhibits the enzyme adenylate cyclase. Inactivation of adenylate cyclase in turn leads to the inactivation of the secondary messenger cyclic adenosine monophosphate and induces smooth muscle and blood vessel constriction. Classes Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity. NB: the inclusion of a drug in each cat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carmoxirole
Carmoxirole (; developmental code name EMD-45609) is a dopamine D2 receptor agonist which was developed as a potential antihypertensive and heart failure medication but was never marketed. It is taken orally. Pharmacology Carmoxirole is a potent, selective, and peripherally restricted partial agonist of the dopamine D2 receptor. It showed about 1,000-fold higher affinity for the dopamine D2 receptor over the dopamine D1 receptor. Carmoxirole also showed some affinity for the serotonin 5-HT1A receptor and for the α2-adrenergic receptor, whereas affinity for other receptors like the serotonin 5-HT2, α1-adrenergic, and β-adrenergic receptors was negligible. The drug has been found to reverse hyperprolactinemia induced by the dopamine D2 receptor antagonist amisulpride without producing central effects in rats. It has also been found to reduce circulating norepinephrine levels by 55% in people with severe heart failure, an action thought to be mediated by its dopamine D ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
7-OH-DPAT
7-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with reasonable selectivity for the D3 receptor subtype, and low affinity for serotonin receptors, unlike its structural isomer 8-OH-DPAT. 7-OH-DPAT is self-administered in several animal models, and is used to study its addiction effects to cocaine. See also * 5-OH-DPAT * 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor, 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonis ... * PD-128,907 * Rotigotine * UH-232 References 2-Aminotetralins Dipropylamino compounds Hydroxyarenes Dopamine agonists {{alkanederivative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-OH-DPAT
5-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with selectivity for the D2 receptor and D3 receptor subtypes. Only the (''S'')-enantiomer is active as an agonist, with the (''R'')-enantiomer being a weak antagonist at D2 receptors. Radiolabelled 11C-5-OH-DPAT is used as an agonist radioligand for mapping the distribution and function of D2 and D3 receptors in the brain, and the drug is also being studied in the treatment of Parkinson's disease. See also * 7-OH-DPAT * 8-OH-DPAT 8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT1A receptor, 5-HT1A receptor. It was one of the first major 5-HT1A receptor full agonis ... References 2-Aminotetralins Dipropylamino compounds Hydroxyarenes Dopamine agonists {{alkanederivative-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rotigotine
Rotigotine, sold under the brand name Neupro among others, is a dopamine agonist of the non- ergoline class of medications indicated for the treatment of Parkinson's disease and restless legs syndrome. It is formulated as a once-daily transdermal patch which provides a slow and constant supply of the drug over the course of 24 hours. Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well. Side effects General side effects for rotigotine may include constipation, dyskinesia, nausea, vomiting, dizziness, fatigue, insomnia, somnolence, confusion, and hallucinations. More serious complications can include psychosis and impulse-control disorders like hypersexuality, punding, and pathological gambling. Mild adverse skin reactions at the patch application site may also occur. Pharmacology Rotigotine acts as a non-selective agonist of the dopamine D1, D2, D3, and, to a lesser extent, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
