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Noradrenergic And Specific Serotonergic Antidepressant
Noradrenergic and specific serotonergic antidepressants (NaSSAs) are a class of psychiatric drugs used primarily as antidepressants. They act by antagonizing the α2-adrenergic receptor and certain serotonin receptors such as 5-HT2A and 5-HT2C, but also 5-HT3, 5-HT6, and/or 5-HT7 in some cases. By blocking α2-adrenergic autoreceptors and heteroreceptors, NaSSAs enhance adrenergic and serotonergic neurotransmission in the brain involved in mood regulation, notably 5-HT1A-mediated transmission. In addition, due to their blockade of certain serotonin receptors, serotonergic neurotransmission is not facilitated in unwanted areas, which prevents the incidence of many side effects often associated with selective serotonin reuptake inhibitor (SSRI) antidepressants; hence, in part, the "specific serotonergic" label of NaSSAs. List of NaSSAs The NaSSAs include the following agents: * Aptazapine (CGS-7525A) * Esmirtazapine (ORG-50,081) * Mianserin (Bolvidon, Norval, Tolvon) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mirtazapine
Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to four weeks but can also manifest as early as one to two weeks. It is often used in cases of depression complicated by anxiety or insomnia. The effectiveness of mirtazapine is comparable to other commonly prescribed antidepressants. It is taken oral administration, by mouth. Common side effects include somnolence, sleepiness, vertigo, dizziness, hyperphagia, increased appetite, and weight gain. Serious side effects may include mania, neutropenia, low white blood cell count, and increased suicide among children. Drug withdrawal, Withdrawal symptoms may occur with stopping. It is not recommended together with a monoamine oxidase inhibitor, although evidence supporting the danger of this combination has been challenged. It is unclear if use during pregnancy i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mood (psychology)
In psychology, a mood is an affective state. In contrast to emotions or feelings, moods are less specific, less intense and less likely to be provoked or instantiated by a particular stimulus or event. Moods are typically described as having either a positive or negative valence. In other words, people usually talk about being in a good mood or a bad mood. There are many different factors that influence mood, and these can lead to positive or negative effects on mood. Mood also differs from temperament or personality traits which are even longer-lasting. Nevertheless, personality traits such as optimism and neuroticism predispose certain types of moods. Long-term disturbances of mood such as clinical depression and bipolar disorder are considered mood disorders. Mood is an internal, subjective state, but it often can be inferred from posture and other behaviors. "We can be sent into a mood by an unexpected event, from the happiness of seeing an old friend to the anger of d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antihistamine
Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides relief from nasal congestion, sneezing, or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use. Although the general public typically uses the word "antihistamine" to describe drugs for treating allergies, physicians and scientists use the term to describe a class of drug that opposes the activity of histamine receptors in the body. In this sense of the word, antihistamines are subc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
In chemistry, 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 and .The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. \begin \ce;& \quad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
S32212
S32212 is a drug which is under preclinical investigation as a potential antidepressant medicine. It behaves as a selective, combined 5-HT2C receptor inverse agonist and α2-adrenergic receptor antagonist (at all three subtypes— α2A, α2B, and α2C) with additional 5-HT2A and, to a lesser extent, 5-HT2B receptor antagonistic properties, and lacks any apparent affinity for the monoamine reuptake transporters or for the α1-adrenergic, H1, or mACh receptors. This profile of activity is compatible with the definition of a noradrenergic and specific serotonergic antidepressant (NaSSA), and as such, S32212 could in turn be classified as a NaSSA. In animal studies, S32212 raised BDNF concentrations in the hippocampus and amygdala, increased the firing rate of neurons in the adrenergic perikarya in the locus coeruleus, increased levels of norepinephrine in the frontal cortex and hippocampus, and elevated frontal cortex levels of dopamine and acetylcholine, though not of s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Structure
A chemical structure of a molecule is a spatial arrangement of its atoms and their chemical bonds. Its determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid. Molecular geometry refers to the spatial arrangement of atoms in a molecule and the chemical bonds that hold the atoms together and can be represented using structural formulae and by molecular models; complete electronic structure descriptions include specifying the occupation of a molecule's molecular orbitals. Structure determination can be applied to a range of targets from very simple molecules (e.g., diatomic oxygen or nitrogen) to very complex ones (e.g., such as protein or DNA). Background Theories of chemical structure were first developed by August Kekulé, Archibald Scott Couper, and Aleksandr Butlerov, among others, from about 1858. These theories were first to state that chemical compounds are not a ran ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tetracyclic Antidepressant
Tetracyclic antidepressants (TeCAs) are a class of antidepressants that were first introduced in the 1970s. They are named after their tetracyclic chemical structure, containing four cyclic compound, rings of atoms, and are closely related to the tricyclic antidepressants (TCAs), which contain three rings of atoms. List of TeCAs Marketed * Maprotiline (Ludiomil) – can also be classified as a TCA and grouped with the secondary amines * Mianserin (Tolvon) * Mirtazapine (Remeron) * Setiptiline (Tecipul) Drugs that contain four rings not all fused together but are sometimes still classified as TeCAs include: * Amoxapine (Asendin) – often classified as a TCA and grouped with the secondary amines * Quetiapine (Seroquel) - an atypical antipsychotic sometimes used as an adjunct antidepressant Miscellaneous * Benzoctamine (Tacitin) – a tetracyclic compound and is closely related to maprotiline, with the two compounds differing only in the length of their side chain, but benzocta ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Setiptiline
Setiptiline (brand name Tecipul), also known as teciptiline, is a tetracyclic antidepressant (TeCA) that acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). It was launched in 1989 for the treatment of depression in Japan by Mochida. Pharmacology Pharmacodynamics Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2 subtypes, as well as an H1 receptor inverse agonist/antihistamine. Chemistry Setiptiline has a tetracyclic structure and is a close analogue of mianserin and mirtazapine, with setiptiline being delta(13b,4a),4a-carba-mianserin, and mirtazapine being 6-azamianserin. See also * Aptazapine * Mianserin * Mirtazapine Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mianserin
Mianserin, sold under the brand name Tolvon among others, is an atypical antidepressant that is used primarily in the treatment of depression in Europe and elsewhere in the world. It is a tetracyclic antidepressant (TeCA). Mianserin is closely related to mirtazapine, both chemically and in terms of its actions and effects, although there are significant differences between the two drugs (for example, its higher noradrenergic activity and lower 5-HT3 receptor antagonism). Medical uses Mianserin at higher doses (30–90 mg/day) is used for the treatment of major depressive disorder. It can also be used at lower doses (around 10 mg/day) to treat insomnia. Contraindications It should not be given, except if based on clinical need and under strict medical supervision, to people younger than 18 years old, as it can increase the risk of suicide attempts and suicidal thinking, and it can increase aggressiveness. While there is no evidence that it can harm a fetus fr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Esmirtazapine
Esmirtazapine (ORG-50,081) is a tetracyclic antidepressant drug that was under development by Organon for the treatment of insomnia and vasomotor symptoms (e.g., hot flashes) associated with menopause. Esmirtazapine is the (''S'')-(+)-enantiomer of mirtazapine and possesses similar overall pharmacology, including inverse agonist actions at H1 and 5-HT2 receptors and antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.α2-adrenergic receptors. Notably, esmirt ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aptazapine
Aptazapine (developmental code name CGS-7525A) is a tetracyclic antidepressant (TeCA) that was assayed in clinical trials for the treatment of depression in the 1980s but was never marketed. It is a potent α2-adrenergic receptor antagonist with about 10 times the strength of the related compound mianserin and has also been shown to act as a 5-HT2 receptor antagonist and H1 receptor inverse agonist, while having no significant effects on the reuptake of serotonin or norepinephrine. Based on its pharmacological profile, aptazapine may be classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). See also * Mianserin * Mirtazapine Mirtazapine, sold under the brand name Remeron among others, is an atypical antidepressant, atypical tetracyclic antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to four weeks but ca ... * Setiptiline References External links * {{Tricyclics Abandoned dru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
