Amines tranquilizers

UPS results are also available for the amino acids and their methyl esters, peptides, porphyrins, steroids, vitamins, opiate narcotics, biogenic amines, tranquilizers, antipyretic and antiinflammatory agents, quinonoid molecules (which are important for electron... 

Next the product is acylated with bromoacetyl chloride and the glycine equivalent is constructed in place by a Gabriel amine synthesis (phthalamide anion followed by hydrazine) subsequent to which cyclization to benzodiazepine occurs. The synthesis of the tranquilizer quazepam (88) is finished by thioamide conversion with phosphorus pentasulfide. ... 

A number of benzodiazepines have heterocyclic rings anne-lated to them. One such is the tranquilizer midazol am (94). Nitrosation (HONO) of secondary amine leads to the ] -nitroso analogue Nitrosoamidines, in the presence of carbanions,... 

Many alkaloids have pronounced biological properties, and a substantial number of the pharmaceutical agents used today are derived from naturally occurring amines. As a few examples, morphine, an analgesic agent, is obtained from the opium poppy Papaver somnifemm. Cocaine, both an anesthetic and a central nervous system stimulant, is obtained front the coca bush Erythroxylon coca, endemic to upland rain forest areas of Colombia, Ecuador, Peru, Bolivia, and western Brazil. Reserpine, a tranquilizer and antihypertensive, comes from powdered roots of the semitropical plant Rauwolfia serpentina. Ephedrine, a bronchodilator and decongestant, is obtained front the Chinese plant Ephedra sinica. 

In 1960, the sedative, muscle-relaxing and anticonvulsant properties of 7-chloro-tV-methyl-5-phenyl-3//-l, 4-benzodiazcpin-2-amine 4-oxide ( chlordiazepoxide ) led to its introduction into clinical use as the active ingredient of the tranquilizer Librium . 

Azaperone (128) is yet another of the tranquilizers related to haloperidol. Nucleophilic aromatic displacement of 2-chloropyridine by piperazine leads to amine 126 which is then alkylated in turn by 4-chloro-p-fluorobuterophenone (127) to give... 

Other plants known to contain psychoactive compounds include hellebore, which was used for centuries in Europe to treat mania, violent temper, mental retardation and epilepsy. However, a drug of major importance in modern psychopharmacology arose from the discovery by medicinal chemists of the alkaloids of Rauwolfia serpentina, a root which had been used in the Indian subcontinent for centuries, not only for the treatment of snake bite but also for alleviating "insanity". Understandably, the mechanism of action of reserpine, the alkaloid purified from Rauwolfia serpentina, helped to lay the basis to psychopharmacology by demonstrating how the depletion of central and peripheral stores of biogenic amines was correlated with a reduction in blood pressure and tranquillization. 

Another CNS active agent in this structural class is the tranquilizer-antidepressant caroxazone (52). Its published synthesis begins by reductive amination of salicylaldehyde and glycinamide to give The synthesis is completed by reaction with phosgene and sodium bicarbonate. ... 

Tricyclic antidepressants, major tranquillizers used in mental hospitals, are separated at UV, 254 nm, on Ci8 using 55% An/water at pH 5.5 with pentane sulfonate. Since these are very basic compounds, it is necessary to use hybrid or heavily end-capped columns and their separation benefits from organic modifiers, such as nonyl amine. 

Active Constituents D-lysergic acid amine and related compounds. Effects LSD-like experience with extreme lassitude. Nausea may be experienced during first hour or two. Total experience lasta bout 6 hours. Tranquil feelings may continue for 12 or more hours afterwards. 

In many reactions the simple saturated nitrogen heterocycles—piperidine, pyrrolidine, piperazine, and morpholine—behave simply as secondary amines that happen to be cyclic. They do the sorts of things that other amines do, acting as nucleophiles in addition and substitution reactions. Morpholine, for example, is acylated by 3,4,5-trimethoxybenzoyl chloride to form the tranquillizer and muscle relaxant trimetozine, and N-methyl piperazine can be alkylated in an S l reaction with diphenylmethyl chloride to give the travel-sickness drug cyclizine. 

Reserpine. As mentioned earlier, the Rauwolfia alkaloid reserpine is noted for its ability to deplete aromatic biogenic amines in nervous tissue of mammals and insects. One of the more remarkable effects of reserpine in humans is to render individuals indifferent to environmental stimuli. Reserpine appears to have a similar effect on insects, although information is still relatively scanty. In the cockroach, Periplaneta americana, reserpine at 50 vg/g causes strong and long-lasting depletion of the aromatic biogenic amines dopamine, octopamine, and 5-hydroxytryptamine (24). Numerous authors have noted that reserpine has tranquilizing effects on insects, e.g., the ant Formica rufa (30) and . americana (24,31). 

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