Opiates morphine

Opiates iateract with three principal classes of opioid GPCRs )J.-selective for the endorphiQS,5-selective for enkephalins, and K-selective for dynorphias (51). AU. three receptors have been cloned. Each inhibits adenylate cyclase, can activate potassium channels, and inhibit A/-type calcium channels. The classical opiates, morphine and its antagonists naloxone (144) and naltrexone (145), have moderate selectivity for the. -receptor. Pharmacological evidence suggests that there are two subtypes of the. -receptor and three subtypes each of the 5- and K-receptor. An s-opiate receptor may also exist. 

Opiates (morphine, codeine, cocaine, etc.) EMIT Syva Corporation http //syva.com... 

Codeine (12) and morphine (13), both major active constituents of opium resin, the dried latex from the immature fruits of Papaver som-niferum L., are pharmacologically important drugs as analgesic agents with considerable use today. Like other opiates, morphine and codeine... 

Figure 3.7 The binding sites and pathways (in red) of opiate (morphine-type) drugs, in the brainstem (rightmost two red spheres), sites invoived in the transmission of pain inciude the nucieus raphe magnus and iocus ceruieus, with other nuciei in the hypothaiamus and thaiamus (spheres to the ieft). Nerve pathways (red) extend to the frontai cortex (far ieft) and up into the iimbic system (center-ieft). Kairos, Latin Stock/Photo Researchers, inc.

The alkaloids derived from opium are collectively known as opiates. Morphine, codeine, and thebaine are well-known opium derivatives. Paregoric is an opium tincture (opium in an alcohol mixture). 

The characterisation and quantification of opiates (morphine, 6-MAM, codeine, and ethylmorphine) are obtained with the aid of a GC/MS. The apparatus and the conditions used are the following ... 

Up to the late 1950s the goal of potency in the development of novel analgesics was that of the classic opiate morphine. However, in 1957 it was made apparent from reports from CIBA on analgesics based on benzimidazole that levels of activity several orders above this standard could be achieved, and the group is of historical importance on this account.(1,2) The compounds of general formula 3 carry a 2-aminoethyl substituent at N-l and a benzyl substituent at C-2 with further substituents at C-5 and C-4 in the more potent derivatives. Two synthetic routes were employed (Scheme 11.1)<3) (a) condense... 

Opiates (morphine, heroin, codeine, etc., SPE) Opiates (morphine, heroin, codeine, amphetamine, caffeine)... 

The enkephalins, H—Tyr—Gly—Gly—Phe—X—OH (X=Leu, Met), or so-called opioid peptides because they mimic the action of the opiates, morphine and heroin, have a very short half life in the body because all four peptide bonds are prone to undergoing proteolysis. The Tyr—Gly bond can be hydrolysed by amino-peptidases, the Gly—Gly bond by dipeptidylaminopeptidases, the Gly—Phe bond by enkephalinase and the Phe—Met and Phe—Leu bonds by carboxypeptidases. An enormous number of analogues have been synthesised, especially with the object of producing compounds that exert potent analgaesic action but are free from side effects. Protection of the susceptible bonds by changing the amino-acid sequence is the obvious way to achieve this. The analogue H—Tyr—d—Met—Gly—Phe—... 

The observation that morphine inhibits c-AMP formation stimulated by PGE- led to the hypothesis that inhibition of a prostaglandin-sensitive adenyl cyclase forms the biochemical basis of the analgesic action of opiates. Morphine also prevents PGE- -mediated inhibition of the aggregation of human platelets and the positive chronotropic effects of PGE- and PGE2 on guinea pig atria . Similar to morphine, leucine- and methionine enkephalin inhibit PGE1 stimulated c-AMP formation in hybrid... 

Cough suppressants have been traditionally divided into the central acting ones that include the opiates morphine, diamorphine, pholcodeine, and codeine, as being... 

Cannabis is by far the most commonly used illicit drug. Most people who abuse hard drugs such as heroin also abuse cannabis. Tetrahydrocannabinol (acid and A -metabolite) is regulated in the German traffic law (see Table 7-1), and amphetamine, opiates (morphine) and cocaine (as benzoylecgonine metabolite) are also mentioned. 

The compound methadone (66) appears to have the structural features needed to bind to opiate receptors in the brain. This compound is active orally. Naturally occurring peptides called enkephalins (67 and 68) have been isolated from brain tissues of certain animals, including man (Fig. 32.21). These compounds are derived from larger peptides. Both have analgesic effects and apparently act at the same receptors as opiates. Morphine and related alkaloids may also occur in animal tissues (Kosterlitz, 1987). 

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