|
3-Quinuclidinyl Thiochromane-4-carboxylate
3-Quinuclidinyl thiochromane-4-carboxylate is a research compound which is the most potent muscarinic antagonist known. Tests ''in vitro'' showed it to have a binding affinity over 2100 times more potent than 3-quinuclidinyl benzilate (BZ) with an apparent association constant (KA) of 2.47 picomolar (pM). See also * CS-27349 * EA-3167 * Metixene Metixene (brand names Methixart, CholinFall, Tremonil, Trest), also known as methixene, is an anticholinergic used as an antiparkinsonian agent. It has also been reported to induce incomplete autophagy and cell death in metastatic cancer and brai ... References Muscarinic antagonists Thiochromanes 3-Quinuclidinyl esters {{psychoactive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Antagonist
A muscarinic acetylcholine receptor antagonist, also simply known as a muscarinic antagonist or as an antimuscarinic agent, is a type of anticholinergic drug that blocks the activity of the muscarinic acetylcholine receptors (mAChRs). The muscarinic receptors are proteins involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the central and peripheral nervous systems. Drugs with muscarinic antagonist activity are widely used in medicine, i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
In Vitro
''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in biology and its subdisciplines are traditionally done in labware such as test tubes, flasks, Petri dishes, and microtiter plates. Studies conducted using components of an organism that have been isolated from their usual biological surroundings permit a more detailed or more convenient analysis than can be done with whole organisms; however, results obtained from ''in vitro'' experiments may not fully or accurately predict the effects on a whole organism. In contrast to ''in vitro'' experiments, ''in vivo'' studies are those conducted in living organisms, including humans, known as clinical trials, and whole plants. Definition ''In vitro'' (Latin language, Latin for "in glass"; often not italicized in English usage) studies are conducted ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Association Constant
The binding constant, or affinity constant/association constant, is a special case of the equilibrium constant ''K'', and is the inverse of the dissociation constant. It is associated with the binding and unbinding reaction of receptor (R) and ligand (L) molecules, which is formalized as: :R + L RL The reaction is characterized by the on-rate constant ''k''on and the off-rate constant ''k''off, which have units of M−1 s−1 and s−1, respectively. In equilibrium, the forward binding transition R + L → RL should be balanced by the backward unbinding transition RL → R + L. That is, :k_\,[]\,[] = k_\,[], where [R], [L] and [RL] represent the concentration of unbound free receptors, the concentration of unbound free ligand and the concentration of receptor-ligand complexes. The binding constant ''K''a is defined by :K_ = = . An often considered quantity is the dissociation constant ''K''d ≡ , which has the unit of concentration, despite the fact that st ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Picomolar
Molar concentration (also called molarity, amount concentration or substance concentration) is the number of moles of solute per liter of solution. Specifically, It is a measure of the concentration of a chemical species, in particular, of a solute in a solution, in terms of amount of substance per unit volume of solution. In chemistry, the most commonly used unit for molarity is the number of moles per liter, having the unit symbol mol/L or mol/ dm3 (1000 mol/ m3) in SI units. A solution with a concentration of 1 mol/L is said to be 1 molar, commonly designated as 1 M or 1 M. Molarity is often depicted with square brackets around the substance of interest; for example, the molarity of the hydrogen ion is depicted as + Definition Molar concentration or molarity is most commonly expressed in units of moles of solute per litre of solution. For use in broader applications, it is defined as amount of substance of solute per unit volume of solution, or per u ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CS-27349
CS-27349, or L-2-α-tropinyl benzilate, is an experimental incapacitating agent. It acts as an antagonist to muscarinic acetylcholine receptors, causing delirium. It has 37% of the potency of the related compound 3-quinuclidinyl benzilate (BZ) in producing peripheral effects, but 85% of the potency in producing central effects. The mean dose required to incapacitate subjects was 1.2 times that of BZ. It has not been in use since the 1970s, and there have been no publications about its effects or long-term toxicology since then. Reference: Patent: It is interesting to notice that 2-tropinone is made from cocaine Cocaine is a tropane alkaloid and central nervous system stimulant, derived primarily from the leaves of two South American coca plants, ''Erythroxylum coca'' and ''Erythroxylum novogranatense, E. novogranatense'', which are cultivated a ... alkaloid. On a related note, it is worthy of mention that 2-tropinone has also had use in the synthesis of isohomoepib ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
EA-3167
EA-3167 is a potent and long-lasting anticholinergic deliriant drug, related to the chemical warfare agent 3-quinuclidinyl benzilate (QNB) and to the bronchodilator drug tiotropium bromide. It was developed under contract to Edgewood Arsenal during the 1960s as part of the US military chemical weapons program, in an attempt to develop non-lethal incapacitating agents. EA-3167 has identical effects to QNB (EA-2277), but is even more potent and longer-lasting, with an effective dose when administered by injection of as little as 2.5 μg/kg (i.e. 0.2 milligrams for an 80 kg person), and a duration of 120–240 hours (5–10 days). However unlike QNB, EA-3167 was never weaponized or manufactured in bulk. Stereoisomers of EA-3167 have also been synthesized under the codename HL-031120. Effects Incapacitating effects can last anywhere from 5-10 days, sometimes manifesting as a full 3-day peak of vivid hallucinations, along with prolonged confusion, amnesia, and inhibition o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metixene
Metixene (brand names Methixart, CholinFall, Tremonil, Trest), also known as methixene, is an anticholinergic used as an antiparkinsonian agent. It has also been reported to induce incomplete autophagy and cell death in metastatic cancer and brain metastases. See also * 3-Quinuclidinyl thiochromane-4-carboxylate *Dothiepin Dosulepin, also known as dothiepin and sold under the brand name Prothiaden among others, is a tricyclic antidepressant (TCA) which is used in the treatment of depression. Dosulepin was once the most frequently prescribed antidepressant in the ... References Antiparkinsonian agents Muscarinic antagonists Thioxanthenes Piperidines {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Antagonists
A muscarinic acetylcholine receptor antagonist, also simply known as a muscarinic antagonist or as an antimuscarinic agent, is a type of anticholinergic drug that blocks the activity of the muscarinic acetylcholine receptors (mAChRs). The muscarinic receptors are proteins involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the central and peripheral nervous systems. Drugs with muscarinic antagonist activity are widely used in medicine, i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
