CE-LAD
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CE-LAD
CE-LAD, or CHLORETH-LAD, also known as 6-(2-chloroethyl)-LAD or 6-(2-chloroethyl)-6-nor-LSD, is a compound of the lysergamide family related to the serotonergic psychedelic lysergic acid diethylamide (LSD). It was developed by psychedelic chemist David E. Nichols at UNC-Chapel Hill (formerly Purdue University) for potential use in scientific research. The compound is an analogue of LSD and ETH-LAD (6-ethyl-6-nor-LSD) in which the 6-position ''N''-alkyl chain has been replaced with a nitrogen mustard 2-chloro ethyl group. Nichols developed CE-LAD in hopes that it would be an alkylating irreversible ligand of a mutant serotonin 5-HT2A receptor that could help facilitate study of serotonin 5-HT2A protein–ligand complexes. CE-LAD was said by journalist Hamilton Morris to have been one of Nichols's final creations prior to his full retirement. It was described by Morris in 2021 in the final episode of his TV show ''Hamilton's Pharmacopeia''. Nichols related that the compound ...
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Substituted Lysergamide
Lysergamides, also known as ergoamides or as lysergic acid amides, are amides of lysergic acid (LA). They are ergolines, with some lysergamides being found naturally in ergot as well as other fungi. Lysergamides are notable in containing embedded phenethylamine and tryptamine moieties within their ergoline ring system. The simplest lysergamides are ergine (lysergic acid amide; LSA) and isoergine (iso-lysergic acid amide; iso-LSA). In terms of pharmacology, the lysergamides include numerous serotonin and dopamine receptor agonists, most notably the psychedelic drug lysergic acid diethylamide (LSD) but also a number of pharmaceutical drugs like ergometrine, methylergometrine, methysergide, and cabergoline. Various analogues of LSD, such as the psychedelics ALD-52 (1A-LSD), ETH-LAD, LSZ, and 1P-LSD and the non-hallucinogenic 2-bromo-LSD (BOL-148), have also been developed. Ergopeptines like ergotamine, dihydroergotamine, and bromocriptine are also lysergamides, but with a ...
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FLUORETH-LAD
FLUORETH-LAD (TRALA-15), or FE-LAD, also known as 6-(2-fluoroethyl)-LAD or 6-(2-fluoroethyl)-6-nor-LSD, is a lysergamide derivative. It was first proposed by Alexander and Ann Shulgin in their book ''TiHKAL'', but was never synthesised by Shulgin. Synthesis and activity data for the compound were first reported in a 2022 patent by Matthias Grill, in which pharmacological testing showed it to have similar affinity to LSD at some targets such as the 5-HT1A and 5-HT2A serotonin receptors, but much lower affinity at other targets such as 5-HT2C and at dopamine receptors, giving it comparatively greater selectivity compared to LSD. Currently new lysergamide derivates are in the development phase at MiHKAL GmbH in Switzerland. See also * CE-LAD * AL-LAD * ETH-LAD * PRO-LAD PRO-LAD, also known as 6-propyl-6-nor-LSD, is a psychedelic drug of the lysergamide family related to lysergic acid diethylamide (LSD). Use and effects PRO-LAD was described by Alexander Shulgin in his book ''TiH ...
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Hamilton Morris
Hamilton Morris (born April 14, 1987) is an American journalist, documentarian, and scientific researcher. He is the creator and director of the television series ''Hamilton's Pharmacopeia'', in which he investigated the chemistry, history, and cultural impact of various psychoactive drugs. Morris is considered to be one of the world's leading drug journalists. Biography Hamilton Morris was born in New York City, the son of Julia Sheehan, an art historian, and documentary filmmaker Errol Morris. He was raised in Cambridge, Massachusetts. As a teenager, Morris appeared in television commercials, notably a 2002 advertisement for the first-generation iPod. He attended the University of Chicago and The New School, where he studied anthropology and chemistry. He earned a bachelor of science (BSc) degree in liberal arts from The New School. Morris's interest in psychoactive substances blossomed in his late teens when he began reading pharmacology information hosted on websites su ...
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Alkylating Agent
Alkylation is a chemical reaction that entails transfer of an alkyl group. The alkyl group may be transferred as an alkyl carbocation, a free radical, a carbanion, or a carbene (or their equivalents). Alkylating agents are reagents for effecting alkylation. Alkyl groups can also be removed in a process known as dealkylation. Alkylating agents are often classified according to their nucleophilic or electrophilic character. In oil refining contexts, alkylation refers to a particular alkylation of isobutane with olefins. For upgrading of petroleum, alkylation produces a premium blending stock for gasoline. In medicine, alkylation of DNA is used in chemotherapy to damage the DNA of cancer cells. Alkylation is accomplished with the class of drugs called alkylating antineoplastic agents. Nucleophilic alkylating agents Nucleophilic alkylating agents deliver the equivalent of an alkyl anion ( carbanion). The formal "alkyl anion" attacks an electrophile, forming a new covalent bond b ...
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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 ...
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Affinity (pharmacology)
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from Latin ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition o ...
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Chemical Synthesis
Chemical synthesis (chemical combination) is the artificial execution of chemical reactions to obtain one or several products. This occurs by physical and chemical manipulations usually involving one or more reactions. In modern laboratory uses, the process is reproducible and reliable. A chemical synthesis involves one or more compounds (known as '' reagents'' or ''reactants'') that will experience a transformation under certain conditions. Various reaction types can be applied to formulate a desired product. This requires mixing the compounds in a reaction vessel, such as a chemical reactor or a simple round-bottom flask. Many reactions require some form of processing (" work-up") or purification procedure to isolate the final product. The amount produced by chemical synthesis is known as the '' reaction yield''. Typically, yields are expressed as a mass in grams (in a laboratory setting) or as a percentage of the total theoretical quantity that could be produced based ...
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Protein–ligand Complex
A protein–ligand complex is a complex of a protein bound with a ligand (biochemistry), ligand that is formed following molecular recognition between proteins that interact with each other or with other molecules. Formation of a protein-ligand complex is based on molecular recognition between biological macromolecules and ligands, where ligand means any molecule that binds the protein with high affinity and specificity. Molecular recognition is not a process by itself since it is part of a functionally important mechanism involving the essential elements of life like in self-replication, metabolism, and information processing (psychology), information processing. For example DNA replication, DNA-replication depends on recognition and binding of DNA double helix by helicase, DNA single strand by DNA polymerase, DNA-polymerase and DNA segments by DNA ligase, ligase. Molecular recognition depends on Affinity (pharmacology), affinity and Chemical specificity, specificity. Specificity m ...
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Mutant Protein
A mutant protein is the protein product encoded by a gene with mutation. Mutated protein can have single amino acid change (minor, but still in many cases significant change leading to disease) or wide-range amino acid changes by e.g. truncation of C-terminus after introducing premature stop codon. See also * Site-directed mutagenesis * Phi value analysis * missense mutation * nonsense mutation * point mutation * frameshift mutation * silent mutation * single-nucleotide polymorphism In genetics and bioinformatics, a single-nucleotide polymorphism (SNP ; plural SNPs ) is a germline substitution of a single nucleotide at a specific position in the genome. Although certain definitions require the substitution to be present in a ... References Proteins Mutation {{protein-stub ...
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Functional Group
In organic chemistry, a functional group is any substituent or moiety (chemistry), moiety in a molecule that causes the molecule's characteristic chemical reactions. The same functional group will undergo the same or similar chemical reactions regardless of the rest of the molecule's composition. This enables systematic prediction of chemical reactions and behavior of chemical compounds and the design of chemical synthesis. The Reactivity (chemistry), reactivity of a functional group can be modified by other functional groups nearby. Functional group interconversion can be used in retrosynthetic analysis to plan organic synthesis. A functional group is a group of atoms in a molecule with distinctive Chemical property, chemical properties, regardless of the other atoms in the molecule. The atoms in a functional group are linked to each other and to the rest of the molecule by covalent bonds. For repeating units of polymers, functional groups attach to their Chemical polarity, nonp ...
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Ethyl Group
In organic chemistry, an ethyl group (abbr. Et) is an alkyl substituent with the formula , derived from ethane (). ''Ethyl'' is used in the International Union of Pure and Applied Chemistry The International Union of Pure and Applied Chemistry (IUPAC ) is an international federation of National Adhering Organizations working for the advancement of the chemical sciences, especially by developing nomenclature and terminology. It is ...'s nomenclature of organic chemistry for a saturated two-carbon moiety in a molecule, while the prefix "''eth-''" is used to indicate the presence of two carbon atoms in the molecule. Ethylation Ethylation is the formation of a compound by introduction of the ethyl group. The most widely practiced example of this reaction is the ethylation of benzene with ethylene to yield ethylbenzene, a precursor to styrene, which is a precursor to polystyrene. Approximately 24.7 million tons of ethylbenzene were produced in 1999. :: Many ethyl ...
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Chloro
Chlorine is a chemical element; it has symbol Cl and atomic number 17. The second-lightest of the halogens, it appears between fluorine and bromine in the periodic table and its properties are mostly intermediate between them. Chlorine is a yellow-green gas at room temperature. It is an extremely reactive element and a strong oxidising agent: among the elements, it has the highest electron affinity and the third-highest electronegativity on the revised Pauling scale, behind only oxygen and fluorine. Chlorine played an important role in the experiments conducted by medieval alchemists, which commonly involved the heating of chloride salts like ammonium chloride (sal ammoniac) and sodium chloride ( common salt), producing various chemical substances containing chlorine such as hydrogen chloride, mercury(II) chloride (corrosive sublimate), and . However, the nature of free chlorine gas as a separate substance was only recognised around 1630 by Jan Baptist van Helmont. Carl Wilh ...
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