|
Pertine
The pertines are a group of antipsychotics of the cyclized tryptamine and phenylpiperazine families that includes the following drugs: * Alpertine (WIN-31665) * Milipertine (WIN-18935) * Oxypertine (WIN-18501) * Solypertine (WIN-18413) Oxypertine is known to show high affinity for the serotonin 5-HT2 and dopamine D2 receptors (Ki = 8.6nM and 30nM, respectively) and to also act as a catecholamine depleting agent. Oxypertine, milipertine, and solypertine all antagonize the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals. Some of the pertines, like milipertine and solypertine, are notable in containing an NBOMe-like moiety. The pertines were developed and initially described in the 1960s and 1970s. See also * Cyclized tryptamine * 5-MeO-T-NBOMe * ''N''-Benzyltryptamine * Carmoxirole Carmoxirole (; developmental code name EMD-45609) is a dopamine D2 receptor agonist which was developed as a poten ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oxypertine
Oxypertine, sold under the brand name Oxypertine among others, is an antipsychotic medication of the pertine group which was previously used in the treatment of schizophrenia but is no longer marketed. It was also evaluated for the treatment of anxiety. Pharmacology Pharmacodynamics The drug shows high affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ... for the serotonin 5-HT2 receptor, 5-HT2 and dopamine D2 receptor, D2 receptors (Ki = 8.6nM and 30nM, respectively). It antagonizes the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals. Like reserpine and tetrabenazine, oxypertine depletes catecholamines, though not serotonin, possibly contributing to its antipsychotic effectiveness. Chemistry Chemicall ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpertine
Alpertine (, ; developmental code name WIN-31665) is a drug of the pertine group described as an antipsychotic, neuroleptic, and tranqulizer which was never marketed. Structurally, it is a substituted tryptamine and a piperazinylethylindole. The drug is closely structurally related to other "pertines" including milipertine, oxypertine, and solypertine, which are also tryptamines and piperazinylethylindoles. The related drug oxypertine shows high affinity for the serotonin 5-HT2 and dopamine D2 receptors (Ki = 8.6nM and 30nM, respectively) and is also known to act as a catecholamine depleting agent. Oxypertine, milipertine, and solypertine all antagonize the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals. Conversely however, alpertine was not effective, at least at doses of up to 10mg/kg. ''ortho''-Methoxyphenylpiperazine (oMeOPP) has been said to be a metabolite of the related drugs milipertine and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Solypertine
Solypertine (; developmental code name WIN-18413), also known as solypertine tartrate () in the case of the tartrate salt, is a drug of the pertine group described as an antiadrenergic (or adrenolytic/sympatholytic) and as also potentially possessing neuroleptic properties which was never marketed. Structurally, it is a substituted tryptamine and a piperazinylethylindole. The drug is closely structurally related to other "pertines" including alpertine, milipertine, and oxypertine, which are also tryptamines and piperazinylethylindoles. Solypertine can be synthesized from 5,6-methylenedioxyindole. The related drug oxypertine shows high affinity for the serotonin 5-HT2 and dopamine D2 receptors (Ki = 8.6nM and 30nM, respectively) and is also known to act as a catecholamine depleting agent. Oxypertine, milipertine, and solypertine all antagonize the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals. ''ort ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Milipertine
Milipertine (, ; developmental code name WIN-18935) is a drug of the pertine group described as an antipsychotic, neuroleptic, and tranquilizer which was under development for the treatment of schizophrenia but was never marketed. Structurally, it is a substituted tryptamine and a piperazinylethylindole. The drug is closely structurally related to other "pertines" including alpertine, oxypertine, and solypertine, which are also tryptamines and piperazinylethylindoles. The related drug oxypertine shows high affinity for the serotonin 5-HT2 and dopamine D2 receptors (Ki = 8.6nM and 30nM, respectively) and is also known to act as a catecholamine depleting agent. Oxypertine, milipertine, and solypertine all antagonize the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals. ''ortho''-Methoxyphenylpiperazine (oMeOPP) has been said to be a metabolite of milipertine, as well as of oxypertine and several other dru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-MeO-T-NBOMe
5-MeO-T-NBOMe, also known as 5MT-NBOMe or NBOMe-5-MeO-T, is a psychedelic of the tryptamine family related to the 25-NB (NBOMe) drugs. It has been sold online as a designer drug. Pharmacology 5-MeO-T-NBOMe is a serotonin 5-HT2 receptor agonist and produces the head-twitch response in rodents. However, compared to 25I-NBOMe, the drug is much less potent in producing the head-twitch response (~10-fold) and produces a much weaker maximal response (~25%). 5-MeO-T-NBOMe is many times less potent than comparable phenethylamines such as 25C-NBOMe, but is still a reasonably potent and effective partial agonist for the 5-HT2 family of serotonin receptors. A number of related compounds have also been developed, and in contrast to the phenethylamine counterparts the ''meta''-substituted benzyl derivatives are in many cases more potent than the ''ortho''-substituted benzyl compounds. History 5-MeO-T-NBOMe was described by David E. Nichols and colleagues in 2015. See also * Substituted t ... [...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] |
Drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
N-Benzyltryptamine
''N''-Benzyltryptamine, also known as T-NB or NB-T, is a serotonin receptor modulator of the tryptamine family. It is the ''N''-benzyl derivative of tryptamine. The drug shows affinity for the serotonin 5-HT2 receptors. Its affinities (Ki) were 245nM for the serotonin 5-HT2A receptor, 100nM for the serotonin 5-HT2B receptor, and 186nM for the serotonin 5-HT2C receptor. In terms of activational activities, specifically calcium mobilization, ''N''-benzyltryptamine's () values were 162nM (62%) at the serotonin 5-HT2A receptor and 50nM (121%) at the serotonin 5-HT2C receptor. At the serotonin 5-HT2A receptor, it had higher affinity than tryptamine, but lower activational potency in comparison. In other studies, at the rat serotonin 5-HT2A receptor, ''N''-benzyltryptamine's was 407nM and its was 26%. The drug has been reported to produce serotonergic psychedelic-like effects in early studies in animals. This included hyperthermia and behavioral changes in the open field test. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclized Tryptamine
Substituted tryptamines, or simply tryptamines, also known as serotonin analogues (i.e., 5-hydroxytryptamine analogues), are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino group, amino (NH2) group via an ethyl (−CH2–CH2−) side chain, sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms. Well-known tryptamines include serotonin, an important neurotransmitter, and melatonin, a hormone involved in regulating the sleep-wake cycle. Tryptamine alkaloids are found in fungi, plants and animals; and sometimes used by humans for the neurological or psychotropic effects of the substance. Prominent examples of tryptamine alkaloids include psilocybin (from "psilocybin mushrooms") and dimethyltryptamine, DMT. In South America, dimethyltryptamine is obtained f ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Moiety (chemistry)
In organic chemistry, a moiety ( ) is a part of a molecule that is given a name because it is identified as a part of other molecules as well. Typically, the term is used to describe the larger and characteristic parts of organic molecules, and it should not be used to describe or name smaller functional groups of atoms that chemically react in similar ways in most molecules that contain them. Occasionally, a moiety may contain smaller moieties and functional groups. A moiety that acts as a branch extending from the backbone of a hydrocarbon molecule is called a substituent or side chain, which typically can be removed from the molecule and substituted with others. The term is also used in pharmacology, where an active moiety is the part of a molecule responsible for the physiological or pharmacological action of a drug. Active moiety In pharmacology, an active moiety is the part of a molecule or ion—excluding appended inactive portions—that is responsible for the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
