Alkaloids opiate

Dobrenis K, Makman MH, Stefano GB (1995) Occurrence of the opiate alkaloid-selective p. receptor in mammahan microglia, astrocytes and Kupffer cells. Brain Res 686 239-248 Donahoe RM (2004) Multiple ways that drug abuse might influence AIDS progression clues from a monkey model. J Neuroimmunol 147 28-32... 

The opiate alkaloid, papaverine, from Papaver somniferum is an anti-spasmodic, vasodilator, and smooth muscle relaxant. Its total synthesis has been studied since Pictet and Gams early work in 1909 and has since been followed up by various industrial syntheses up till the early 1950s using important industrial commodities as vanillin, acetovanillone, veratraldehyde (methylvanillin), and homoveratric acid as starting materials (see Figure 4.50). Table 4.23 summarizes the results of the five synthetic plans for this natural product. All are convergent... 

Codeine is one of 40 individual chemical compounds (specifically, alkaloid compounds) found in opium. Only a few of the opiate alkaloids are used medically the analgesics (painkillers) morphine... 

Conjugate addition of organocuprates has seen many applications in complex synthesis. For example, in the preparation of an opiate alkaloid it was necessary to introduce a methyl group at a late stage of the synthesis.110 The transformation of (47) to (48) was successfully carried out with Me2CuLi in a stereoselective manner (equation 51). 

Wert, M. A., and MacDonald, R. L. (1982). Opiate alkaloids antagonize postsynaptic glycine and GABA responses Correlation with convulsant action. Brain Res. 236, 107—119. 

Most studies of the local actions of opioids on the intestinal mucosa have utilized muscle-stripped sheets of ileal mucosa with attached submucosa mounted in Ussing flux chambers. Peptidase-resistant enkephalin derivatives such as DPDPE decrease short-circuit current, an electrical measure of active transepithelial ion transport, across isolated mucosal sheets from the guinea pig ileum [46,127,128], rabbit ileum [129-131], mouse jejunum [132], and pig distal jejunum/ileum [133]. This effect, which occurs after the application of opioid agonists to the serosal aspect of epithelial sheets, is due to an increase in electroneutral salt absorption and a decrease in electrogenic chloride secretion [46,132,133], In contrast to enkephalin derivatives, opiate alkaloids have limited effects on active transepithelial transport of ions [69]. Pretreat-... 

The morphinomimetic peptides react with the same receptors as the opiate alkaloids and presumably represent the endogenous agonists of these receptors. /i-Endorphin, which represents the functionally active molecule, plays a role in the response of the organism to stress stimuli. The analgesic effect in the body can be traced back to the secretion of /1-endorphin. Accordingly, acupuncture, for example, activates the central nervous endorphin system and causes an increase in the endorphin concentration, leading to the elimination of sensitivity to pain. Presumably there are endorphinergic systems in the central nervous system (CNS) in which the endorphins assume a neuro-modulatory function. 

Brown AJ, Lenehan CE, Francis PS, Dunstan DE, Barnett NW. Soluble manganese(IV) as a chemiluminescence reagent for the determination of opiate alkaloids, indoles and analytes of forensic interest. Talanta 2007 71 1951-7. 

The biological activity of epibatidine has not been studied in any detail because of the minute quantities available from the frog Epipedobates tricolor. Its presence as a trace alkaloid and its chromatographic purification were based on the Straub tail response that epibatidine causes in mice. The Straub tail response is characteristic of opiate alkaloids however, unlike that caused by morphine and other opiates, the response caused by epibatidine was not reversed by the opiate antagonist naloxone (765). Epibatidine proved to be a potent analgetic, being manyfold more potent than morphine in the hot plate analgetic assay (765). Epibatidine had very low affinity for opioid receptors (765). 

Why do the opiate alkaloids precipitate from aqueous solution at pH... 

The capsules and stems of Papaver somniferum contain opiate alkaloids essential in medicine. They are classified into two groups, phenanthrene types (morphine, codeine, thebaine) and benzylisoquinoline types [papaverine and noscapine(narcotine)]. These two types of alkaloids show sharply specific pharmacological properties. It is noteworthy that morphinane alkaloids are formed from (-)-(/ )-reticuline, whereas most other alkaloids derive from (-l-)-(5)-re-ticuline 11). 

Molecular imprinting [1] is now an established technique for the creation of polymeric matrices with predetermined affinity for particular substrates. The technique has been used for the creation of substrates with affinities for amino acids, peptides, proteins, nucleotides and nucleosides, carbohydrates, various drugs (e.g. opiates, alkaloids, antibiotics, /1-blockers, tranquillisers) and other bioactive compounds (e.g. enkephalin, steroids, corticosteroids), herbicides, pesticides, as well as metal ions and a number of miscellaneous organic compounds [2-5]. 

Opiates are compounds extracted from the milky latex contained in the unripe seed pods of the opium poppy (Papaver somniferum). Opium, morphine, and codeine are the most important opiate alkaloids found in the opium poppy. Opium was used as folk medicine for hundreds, perhaps thousands of years. In the seventeenth century opium smoking led to major addiction problems. In the first decade of the nineteenth century, morphine was isolated from opium. About 20 years later, codeine, one-fifth as strong as morphine, was isolated from both opium and morphine. In 1898, heroin, an extremely potent and addictive derivative of morphine was isolated. The invention of the hypodermic needle during the mid-nineteenth century allowed opiates to be delivered directly into the blood stream, which increases the effects of these drugs. Synthetically produced drugs with morphine-like properties are called opioids. The terms narcotic, opiate, and opioid are frequently used interchangeably. Some common synthetically produced opioids include meperidine (its trade name is Demerol) and methadone, a drug often used to treat heroin addiction. 

The analysis of heroin samples gives rise to a different set of problems. Heroin contains a mixture of opiate alkaloids and one of these, diamor-phine (diacetylmorphine), is the controlled drug which has to be determined quantitatively. The other major opiates present in heroin can... 

Abstract This review summarizes recent developments in the total synthesis of morphine alkaloids and some of the semisynthetic derivatives. The literature is covered for the period of 5 years after the pubhcation of the last review in 2005. The syntheses that appeared in this period are covered in detail and are placed in the context of all syntheses of opiate alkaloids since the original one pubhshed by Gates in 1952. The introduction covers the historical aspects of total synthesis of these alkaloids. The synthesis of some of the medicinally useful derivatives is reviewed in the last section along with some of the methodology required for then-preparation. 

McCamley K,Ripper JA, Singer RD, Scammells PJ (2003) Efficient N-demethylation of opiate alkaloids using a modified nonclassical Polonovski reaction. J Org Oiem 68 9847-9850... 

Kok G, Ashton TD, Scammells PJ (2009) An improved process for the N-demethylation of opiate alkaloids using an iron(ll) catalyst in acetate buffer. Adv Synth Catal 351 283-286... 

Endogenous and exogenous alkaloids in shrimp, crabs, and barnacles are not studied. They probably are interesting animals from an evolutional point of view, and their chemistry research could lead to a new alkaloid discoveries. Lobsters have a low concentration endogenous opiate alkaloids in their body. These alkaloids are known to modify the channels and working on the nervous system. ... 

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