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4-PhPr-3,5-DMA
4-PhPr-3,5-DMA, also known as 4-(3-phenylpropyl)-3,5-dimethoxyamphetamine, is a serotonin receptor modulator of the phenethylamine and amphetamine families. It is structurally related to the DOx drugs but has one of its methoxy groups in the 3 position instead of 2 position on the phenyl ring and has a bulky substitution at the 4 position of the phenyl ring. The affinities (Ki) of 4-PhPr-3,5-DMA for the serotonin 5-HT2 receptors have been reported to be 4nM for the serotonin 5-HT2A receptor and 40nM for the serotonin 5-HT2C receptor, with approximately 10-fold selectivity for the serotonin 5-HT2A receptor over the serotonin 5-HT2C receptor. Its affinities for the serotonin 5-HT2A and 5-HT2C receptors in the study were approximately 8-fold and 1.6-fold higher than those of DOB, respectively. The drug was a full agonist of the serotonin 5-HT2A receptor in terms of phosphatidylinositol (PI) hydrolysis ( = 109% relative to serotonin). However, in the presence of the serotonin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
3C (psychedelics)
3C (3C-''x''), also known as 4-substituted 3,5-dimethoxyamphetamines, substituted 3,4,5-trimethoxyamphetamine (3,4,5-TMA or TMA-1) analogues, or 3C-scalines, is a general name for the family of psychedelic amphetamines containing methoxy groups at the 3 and 5 positions of the benzene ring. These compounds are analogues of 3,4,5-trimethoxyamphetamine (3,4,5-TMA or TMA-1). The 3C drugs are not the amphetamine counterparts of the 2C drugs, which are 4-substituted 2,5-dimethoxyphenethylamines. Instead, the DOx drugs, which are 4-substituted 2,5-dimethoxyamphetamines, are the amphetamine counterparts of the 2C drugs. The 3C drugs are the amphetamine counterparts of substituted mescaline analogues (4-substituted 3,5-dimethoxyphenethylamines). Moreover, in terms of naming with the "3C" prefix, the 3C drugs are generally actually derivatives of TMA-1 with the 4-position methoxy group extended rather than having any 4-position substituent. In this regard, they would be the 3,5-dime ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
4-PhPr-2,5-DMA
4-(3-Phenylpropyl)-2,5-dimethoxyamphetamine (DOPP or DOPhPr), also known as 4-PhPr-2,5-DMA, is a serotonin receptor modulator of the phenethylamine, amphetamine, and DOx families. It shows high affinity for both the serotonin 5-HT2A and 5-HT2C receptors and acts as a weak partial agonist or antagonist of the serotonin 5-HT2A receptor. The drug has lower affinity for the serotonin 5-HT2A receptor than its closely related positional isomer 4-PhPr-3,5-DMA. This is an apparent reversal of the usual situation with DOx and related drugs in which the 2,5-dimethoxy pattern is optimal for serotonin 5-HT2A receptor interactions. See also * DOBz * 2C-T-27 * 2C-Ph 2C-Ph, also known as 2C-BI-1 or as 2,5-dimethoxy-4-phenylphenethylamine, is a serotonin receptor modulator of the phenethylamine and 2C families that was developed by Daniel Trachsel and David E. Nichols and colleagues. The drug's affinity (Ki) ... * DOHx References External links DOPhPr - Isomer Design 5-HT2A agoni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2,5-dimethoxy-4-bromoamphetamine
Dimethoxybromoamphetamine (DOB), also known as brolamfetamine () and bromo-DMA, is a psychedelic drug and substituted amphetamine of the phenethylamine class of compounds. DOB was first synthesized by Alexander Shulgin in 1967. Its synthesis and effects are documented in Shulgin's book '' PiHKAL: A Chemical Love Story''. The drug acts as a serotonin 5-HT2 receptor agonist. Side effects Excessively high doses of DOB may cause diffuse arterial spasm. The vasospasm responded readily to intra-arterial and intravenous vasodilators, such as tolazoline. Interactions Pharmacology Pharmacodynamics DOB is a serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptor agonist. Its psychedelic effects are mediated by its agonistic properties at the 5-HT2A receptor. Due to its selectivity, DOB is often used in scientific research when studying the 5-HT2 receptor subfamily. It is a very weak agonist of the human trace amine-associated receptor 1 (TAAR1) and a weak agonist of the rhesus ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Psychedelic Drug
Psychedelics are a subclass of hallucinogenic drugs whose primary effect is to trigger non-ordinary mental states (known as psychedelic experiences or "trips") and a perceived "expansion of consciousness". Also referred to as classic hallucinogens or serotonergic hallucinogens, the term ''psychedelic'' is sometimes used more broadly to include various other types of hallucinogens as well, such as those which are atypical or adjacent to psychedelia like salvia and MDMA, respectively. Classic psychedelics generally cause specific psychological, visual, and auditory changes, and oftentimes a substantially altered state of consciousness. They have had the largest influence on science and culture, and include mescaline, LSD, psilocybin, and DMT. There are a large number of both naturally occurring and synthetic serotonergic psychedelics. Most psychedelic drugs fall into one of the three families of chemical compounds: tryptamines, phenethylamines, or lysergamides. T ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves ." '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, beta b ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOHx
2,5-Dimethoxy-4-hexylamphetamine (DOHx or DOHE) is a non-hallucinogenic serotonin receptor modulator of the phenethylamine, amphetamine, and DOx families. Pharmacology DOHx has shown the highest affinity for the serotonin 5-HT2A and 5-HT2C receptors of any other assessed DOx drug in multiple studies. In one study, its affinities for the human serotonin 5-HT2 receptors were 0.1nM for the 5-HT2A receptor, 30nM for the 5-HT2B receptor, and 0.7nM for 5-HT2C receptor. In the case of the serotonin 5-HT2A receptor, this was 6- to 14-fold higher than DOB, DOI, and DOC and was 9-fold higher than DOPR. In another study, DOHx showed 25-fold higher affinity for the serotonin 5-HT2A receptor than DOM or DOET, 23- to 28-fold higher affinity than DOPR and DOBU, and 2.8-fold higher affinity than DOAM. Conversely, it showed only slightly higher or roughly the same affinity for the receptor relative to DOCT (2.5nM vs. 3.0nM, respectively). In contrast to many other DOx drugs, DOHx, as well ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Derivative
In chemistry, a derivative is a compound that is derived from a similar compound by a chemical reaction. In the past, derivative also meant a compound that ''can be imagined to'' arise from another compound, if one atom or group of atoms is replaced with another atom or group of atoms, but modern chemical language now uses the term structural analog for this meaning, thus eliminating ambiguity. The term "structural analogue" is common in organic chemistry. In biochemistry, the word is used for compounds that at least theoretically can be formed from the precursor compound. Chemical derivatives may be used to facilitate analysis. For example, melting point (MP) analysis can assist in identification of many organic compounds. A crystalline derivative may be prepared, such as a semicarbazone or 2,4-dinitrophenylhydrazone (derived from aldehydes or ketones), as a simple way of verifying the identity of the original compound, assuming that a table of derivative MP values is availa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mechanism Of Action
In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical Drug interaction, interaction through which a Medication, drug substance produces its pharmacological effect. A mechanism of action usually includes mention of the specific molecular targets to which the drug binds, such as an enzyme or receptor (biochemistry), receptor. Receptor sites have specific affinities for drugs based on the chemical structure of the drug, as well as the specific action that occurs there. Drugs that do not bind to receptors produce their corresponding therapeutic effect by simply interacting with chemical or physical properties in the body. Common examples of drugs that work in this way are antacids and laxatives. In contrast, a Mode of action, mode of action (MoA) describes functional or anatomical changes, at the cellular level, resulting from the exposure of a living organism to a substance. Importance Elucidating the mechanism of action of novel drugs and medicati ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Partial Agonism
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial agonist actually acts as a competitive antagonist, competing with the full agonist for receptor occupancy and producing a net decrease in the receptor activation observed with the full agonist alone. Clinically, partial agonists can be used to activate receptors to give a desired submaximal response when inadequate amounts of the endogenous ligand are present, or they can reduce the overstimulation of receptors when excess amounts of the endogenous ligand are present. Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine. Examples of ligands activ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bioassay
A bioassay is an analytical method to determine the potency or effect of a substance by its effect on animal testing, living animals or plants (''in vivo''), or on living cells or tissues (''in vitro''). A bioassay can be either quantal or quantitative, direct or indirect. If the measured response is binary, the assay is mwod:quantal, quantal; if not, it is Quantitative research, quantitative. A bioassay may be used to detect biological hazards or to give an assessment of the quality of a mixture. A bioassay is often used to monitor water quality as well as wastewater discharges and its impact on the surroundings. It is also used to assess the environmental impact and safety of new technologies and facilities. Bioassays are essential in pharmaceutical, medical and agricultural sciences for development and launching of new drugs, vitamins, etc. Principle A bioassay is a biochemical test to estimate the potency of a sample compound. Usually this potency can only be measured rela ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ketanserin
Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospasm, vasospastic disorders. It is also used in scientific research as an antiserotonergic medication, agent in the study of the serotonin system; specifically, the 5-HT2 receptor, 5-HT2 receptor family. The drug is taken oral administration, by mouth. Side effects of ketanserin include dizziness, tiredness, edema, dry mouth, weight gain, and drug-induced QT prolongation, QT interval prolongation. Ketanserin acts as a binding selectivity, selective receptor antagonist, antagonist of the serotonin 5-HT2A receptor, 5-HT2A, α1-adrenergic receptor, α1-adrenergic, and histamine H1 receptor, H1 receptors. It also shows lower affinity (pharmacology), affinity for various other biological target, targets. Ketanserin was discovered at Janssen Pharmaceutica in 1980. It was the first serotonin 5-HT2A receptor antagonist to be discovered that showed selectiv ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Silent Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves ." '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include s, |
