|
Perlapine
Perlapine, sold under the brand names Hypnodine and Pipnodine, is a hypnotic and sedative of the tricyclic compound, tricyclic group which is marketed in Japan. It acts primarily as a potency (pharmacology), potent antihistamine, and also has anticholinergic, antiserotonergic, antiadrenergic, and some antidopaminergic activity. The drug has relatively weak affinity (pharmacology), affinity for the dopamine D2 receptor, D2 receptor ( = 1,803 nM) and, in accordance, is said to be ineffective as an antipsychotic. However, it retains higher affinity for the dopamine D1 receptor, D1 receptor ( = 198 nM). Its values are 19 nM for the alpha-1 adrenergic receptor, α1-adrenergic receptor, 4,945 nM for the alpha-2 adrenergic receptor, α2-adrenergic receptor, and 70 nM for the serotonin 5-HT2A receptor, 5-HT2A receptor. Perlapine is closely related to clotiapine, clozapine, fluperlapine, loxapine, and tilozepine. Perlapine has been suggested as a potential ligand ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluperlapine
Fluperlapine (NB 106-689), also known as fluoroperlapine, is a morphanthridine (11''H''-dibenzo ,ezepine) atypical antipsychotic with additional antidepressant and sedative effects. It was first synthesized in 1979, and then subsequently studied in animals and humans in 1984 and beyond, but despite demonstrating efficacy in the treatment of a variety of medical conditions including schizophrenia, psychosis associated with Parkinson's disease, depressive symptoms, and dystonia, it was never marketed. This was perhaps due to its capacity for producing potentially life-threatening agranulocytosis Agranulocytosis, also known as agranulosis or granulopenia, is an acute condition involving a severe and dangerous lowered white blood cell count (leukopenia, most commonly of neutrophils) and thus causing a neutropenia in the circulating blood. ..., similarly to clozapine, which it closely resembles both structurally and pharmacologically. Pharmacology Binding profile Synthe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hypnotic
Hypnotic (from Greek ''Hypnos'', sleep), or soporific drugs, commonly known as sleeping pills, are a class of (and umbrella term for) psychoactive drugs whose primary function is to induce sleep (or surgical anesthesiaWhen used in anesthesia to produce and maintain unconsciousness, "sleep" is metaphorical as there are no regular sleep stages or cyclical natural states; patients rarely recover from anesthesia feeling refreshed and with renewed energy. The word is also used in art.) and to treat insomnia (sleeplessness). This group of drugs is related to sedatives''. ''Whereas the term sedative describes drugs that serve to calm or relieve anxiety, the term hypnotic generally describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness), they are often referred to collectively as sedative- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin
Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vasoconstriction. Approximately 90% of the serotonin that the body produces is in the intestinal tract. Biochemically, the indoleamine molecule derives from the amino acid tryptophan, via the (rate-limiting) hydroxylation of the 5 position on the ring (forming the intermediate 5-hydroxytryptophan), and then decarboxylation to produce serotonin. Serotonin is primarily found in the enteric nervous system located in the gastrointestinal tract (GI tract). However, it is also produced in the central nervous system (CNS), specifically in the raphe nuclei located in the brainstem, Merkel cells located in the skin, pulmonary neuroendocrine cells and taste receptor cells in the tongue. Additionally, serotonin is stored in blood platelets a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
H1 Receptor Antagonists
H1 antagonists, also called H1 blockers, are a class of medications that block the action of histamine at the H1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines; other agents may have antihistaminergic action but are not true antihistamines. In common use, the term "antihistamine" refers only to H1-antihistamines. Virtually all H1-antihistamines function as inverse agonists at the histamine H1-receptor, as opposed to neutral antagonists, as was previously believed. Medical uses H1-antihistamines are clinically used in the treatment of histamine-mediated allergic conditions. These indications may include:Rossi S (Ed.) (2004). ''Australian Medicines Handbook 2004''. Adelaide: Australian Medicines Handbook. * Allergic rhinitis * Allergic conjunctivitis * Allergic dermatological conditions (contact dermatitis) * Rhinorrhea (runny nose) * Urticaria * A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dopamine Antagonists
A dopamine antagonist, also known as an anti-dopaminergic and a dopamine receptor antagonist (DRA), is a type of drug which blocks dopamine receptors by receptor antagonism. Most antipsychotics are dopamine antagonists, and as such they have found use in treating schizophrenia, bipolar disorder, and stimulant psychosis. Several other dopamine antagonists are antiemetics used in the treatment of nausea and vomiting. Receptor pharmacology Dopamine receptors are all G protein–coupled receptors, and are divided into two classes based on which G-protein they are coupled to. The D1-like class of dopamine receptors is coupled to Gαs/olf and stimulates adenylate cyclase production, whereas the D2-like class is coupled to Gαi/o and thus inhibits adenylate cyclase production. D1-like receptors: D1 and D5 D1-like receptors – D1 and D5 are always found post-synaptically. The genes coding these receptors lack introns, so there are no splice variants. D1 receptors * D1 receptors ar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-1 Blockers
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency, a genetic disorder *Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in '' Buzz Lightyear of Star Command: The Adventure Begins'' * ''Alpha 1'' (Robert Silverberg anthology), a 1970 book See also * * *Alpha (other) *AMY1A Alpha-amylase 1 is an enzyme that in humans is encoded by the ''AMY1A'' gene In biology, the word gene (from , ; "... Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth ... or Alpha-1A or, an enzyme found in humans and other mammals * List of A1 genes, proteins or receptors {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Antagonists
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherw ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (for example, infection). Pharmacodynamics and pharmacokinetics are the main branches of pharmacology, being itself a topic of biology interested in the study of the interactions between both endogenous and exogenous chemical substances with living organisms. In particular, pharmacodynamics is the study of how a drug affects an organism, whereas pharmacokinetics is the study of how the organism affects the drug. Both together influence dosing, benefit, and adverse effects. Pharmacodynamics is sometimes abbreviated as PD and pharmacokinetics as PK, especially in combined reference (for example, when speaking of PK/PD models). Pharmacodynamics places particular emphasis on dose–response relationships, that is, the relationships betwe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DREADD
A receptor activated solely by a synthetic ligand (RASSL) or designer receptor exclusively activated by designer drugs (DREADD), is a class of artificially engineered protein receptors used in the field of chemogenetics which are selectively activated by certain ligands. They are used in biomedical research, in particular in neuroscience to manipulate the activity of neurons. Originally differentiated by the approach used to engineer them, RASSLs and DREADDs are often used interchangeably now to represent an engineered receptor-ligand system. These systems typically utilize G protein-coupled receptors (GPCR) engineered to respond exclusively to synthetic ligands, like clozapine N-oxide (CNO), and not to endogenous ligands. Several types of these receptors exists, derived from muscarinic or κ-opioid receptors. Types of RASSLs / DREADDs One of the first DREADDs was based on the human M3 muscarinic receptor (hM3). Only two point mutations of hM3 were required to achieve a mu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Loxapine
Loxapine, sold under the brand names Loxitane and Adasuve (''inhalation'' only) among others, is an antipsychotic medication used primarily in the treatment of schizophrenia. The medicine is a member of the dibenzoxazepine class and structurally very similar to clozapine. Several researchers have argued that loxapine, initially classified as a typical antipsychotic, behaves as an atypical antipsychotic. Loxapine may be metabolized by ''N''-demethylation to amoxapine, a tricyclic antidepressant. Medical uses The US Food and Drug Administration (FDA) has approved loxapine inhalation powder for the acute treatment of agitation associated with schizophrenia or bipolar I disorder in adults. A brief review of loxapine found no conclusive evidence that it was particularly effective in patients with schizophrenia. A subsequent systematic review considered that the limited evidence did not indicate a clear difference in its effects from other antipsychotics. Available forms Loxapine ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
