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Talopram
Talopram (Lu 3-010), also known as phthalapromine, is a selective norepinephrine reuptake inhibitor (NRI) which was researched for the management of depression in the 1960s and 1970s but was never commercialized. Along with talsupram, talopram is structurally related to the selective serotonin reuptake inhibitor (SSRI) citalopram, as well as to melitracen: Synthesis An unexpected/fortuitous rearrangement product in the synthesis of litracen is what led to talopram. See also * Talsupram (tasulopram) * Amedalin * Daledalin *, 1969 (#15). *Original literature *Prindamine Pirandamine (AY-23,713) is a tricyclic derivative which acts as a selective serotonin reuptake inhibitor (SSRI). It was investigated in the 1970s as a potential antidepressant but clinical development was not commenced and it was never marketed. ... (21489-22-5) References Antidepressants Norepinephrine reuptake inhibitors Isobenzofurans {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine Reuptake Inhibitors
A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine and therefore can increase adrenergic neurotransmission. Medical use NRIs are commonly used in the treatment of conditions like ADHD and narcolepsy due to their psychostimulant effects and in obesity due to their appetite suppressant effects. They are also frequently used as antidepressants for the treatment of major depressive disorder, anxiety and panic disorder. Additionally, many addictive substances such as cocaine and methylphenidate possess NRI activity, though NRIs without combined dopamine reuptake inhibitor (DRI) properties are not significantly reward ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Talsupram
Talsupram (Lu 5-005 or Lu 5-003) is a selective norepinephrine reuptake inhibitor (NRI) which was investigated as an antidepressant in the 1960s and 1970s but was never marketed. Along with talopram, it is structurally related to the selective serotonin reuptake inhibitor (SSRI) citalopram.http://www.healyprozac.com/Book/Introduction.doc See also * Talopram Talopram (Lu 3-010), also known as phthalapromine, is a selective norepinephrine reuptake inhibitor (NRI) which was researched for the management of depression in the 1960s and 1970s but was never commercialized. Along with talsupram, talopram ... References Antidepressants Norepinephrine reuptake inhibitors Benzo(c)thiophenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Talsupram
Talsupram (Lu 5-005 or Lu 5-003) is a selective norepinephrine reuptake inhibitor (NRI) which was investigated as an antidepressant in the 1960s and 1970s but was never marketed. Along with talopram, it is structurally related to the selective serotonin reuptake inhibitor (SSRI) citalopram.http://www.healyprozac.com/Book/Introduction.doc See also * Talopram Talopram (Lu 3-010), also known as phthalapromine, is a selective norepinephrine reuptake inhibitor (NRI) which was researched for the management of depression in the 1960s and 1970s but was never commercialized. Along with talsupram, talopram ... References Antidepressants Norepinephrine reuptake inhibitors Benzo(c)thiophenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine Reuptake Inhibitor
A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine and therefore can increase adrenergic neurotransmission. Medical use NRIs are commonly used in the treatment of conditions like ADHD and narcolepsy due to their psychostimulant effects and in obesity due to their appetite suppressant effects. They are also frequently used as antidepressants for the treatment of major depressive disorder, anxiety and panic disorder. Additionally, many addictive substances such as cocaine and methylphenidate possess NRI activity, though NRIs without combined dopamine reuptake inhibitor (DRI) properties are not significantly reward ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Paul Kielholz
Paul Kielholz (15 November 1916 - 25 May 1990) was a Swiss psychiatrist, known mainly for his work on major depression, for example, for his method of overcoming antidepressant resistance by using simultaneous intravenous infusions of clomipramine and maprotiline, together with sulpiride and benzodiazepine Benzodiazepines (BZD, BDZ, BZs), sometimes called "benzos", are a class of depressant drugs whose core chemical structure is the fusion of a benzene ring and a diazepine ring. They are prescribed to treat conditions such as anxiety disorders, ...s. Biography Paul Kielholz was born in 1916 in Switzerland. Scientific works References 1916 births 1990 deaths Swiss psychiatrists {{scientist-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressants
Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common side-effects of antidepressants include dry mouth, weight gain, dizziness, headaches, sexual dysfunction, and emotional blunting. There is a slight increased risk of suicidal thinking and behavior when taken by children, adolescents, and young adults. Discontinuation syndrome may occur after stopping any antidepressant which resembles recurrent depression. Some research regarding the effectiveness of antidepressants for depression in adults has found benefits, whilst other research has not. Evidence of benefit in children and adolescents is unclear. The twenty-one most commonly prescribed antidepressant medications are more effective than placebo for the short-term (acute) treatments of adults with major depressive disorder. There is debate in the medical community about how much of the observed effects of antidepre ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prindamine
Pirandamine (AY-23,713) is a tricyclic derivative which acts as a selective serotonin reuptake inhibitor (SSRI). It was investigated in the 1970s as a potential antidepressant but clinical development was not commenced and it was never marketed. Pirandamine is structurally related to tandamine, which, in contrast, is a selective norepinephrine reuptake inhibitor. Synthesis Condensation of 1-indanone (1) with ethyl bromoacetate and zinc affords Reformatsky reaction product 2; then reduction with LiAlH4 gives diol 3. Dehydration with H2SO4 gives the indene ethanol 4. Acid catalyzed condensation of 4 with ethyl acetoacetate then gives the fused tetrahydropyran derivative 5 (no doubt by a scheme quite analogous to prodolic acid). The ester is then saponified to the corresponding acid, which is then converted to the dimethylamide (6). Reduction with LiAlH4 completes the synthesis of the antidepressant agent pirandamine (7). See also * Tandamine *Prindamine Pirandamine (AY- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Daledalin
Daledalin (UK-3557-15) is an antidepressant which was synthesized and trialed for depression in the early 1970s, but was never marketed. It is a selective norepinephrine reuptake inhibitor, with no significant effects on the reuptake of serotonin and dopamine, and no antihistamine or anticholinergic Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system. These agents inhibit the parasympathetic nervous sys ... properties. Synthesis See also * Amedalin References Abandoned drugs Amines Antidepressants Indolines Norepinephrine reuptake inhibitors {{amine-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Amedalin
Amedalin (UK-3540-1) is an antidepressant which was synthesized in the early 1970s, but was never marketed. It is a selective norepinephrine reuptake inhibitor, with no significant effects on the reuptake of serotonin and dopamine, and no antihistamine or anticholinergic Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system. These agents inhibit the parasympathetic nervous sys ... properties. See also * Daledalin References Abandoned drugs Amines Antidepressants Indolines Gamma-lactams Norepinephrine reuptake inhibitors Oxindoles {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Litracen
Litracen (N-7,049) is a tricyclic antidepressant which was never marketed. See also * Fluotracen * Melitracen Melitracen (brand names Melixeran) is a tricyclic antidepressant (TCA), for the treatment of depression and anxiety. In addition to single drug preparations, it is also available as Deanxit, marketed by Lundbeck, a combination product containi ... References {{Tricyclics Secondary amines Anthracenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
Binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants ''K''AB and ''K''AC.The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. : + B AB; \mathit K_ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lundbeck
H. Lundbeck A/S (commonly known simply as Lundbeck) is a Danish international pharmaceutical company engaged in the research, development, manufacturing, marketing and sale of pharmaceuticals across the world. The company’s products are targeted at brain diseases, including depression, schizophrenia, Alzheimer's disease, Parkinson's disease and migraine. Headquartered in Copenhagen, Denmark, Lundbeck has approximately 5,300 employees in more than 50 countries, and their products are registered in more than 100 countries. They have production facilities in Denmark, France and Italy and their research centers are based in Denmark and the US. Lundbeck is listed on the Copenhagen Stock Exchange (CSE). Lundbeck is a full member of the European Federation of Pharmaceutical Industries and Associations (EFPIA) and of the International Federation of Pharmaceutical Manufacturers and Associations (IFPMA) History The company was founded by Hans Lundbeck in 1915, and was initially a tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
