Pethidine (meperidine). Ketobemidone. MPPP. Allylprodine. Prodine. PEPAP. Promedol. Propoxyphene. Dextropropoxyphene. Dextromoramide. Bezitramide. Piritramide. Methadone. Dipipanone. Levomethadyl Acetate (LAAM). Difenoxin. Diphenoxylate. Loperamide (does cross the blood-brain barrier but is quickly pumped into the non-central nervous system by P-Glycoprotein. Mild opiate withdrawal in animal models exhibits this action after sustained and prolonged use including rhesus monkeys, mice, and rats.). Dezocine—agonist/antagonist. Pentazocine—agonist/antagonist. Phenazocine. Buprenorphine—partial agonist. Dihydroetorphine. Etorphine. Butorphanol—agonist/antagonist. Nalbuphine—agonist/antagonist.
opioidsopioid analgesicendogenous opioids
morphiamorphine addictionmorphine sulfate
The pharmacology of heroin and morphine is identical except the two acetyl groups increase the lipid solubility of the heroin molecule, causing heroin to cross the blood–brain barrier and enter the brain more rapidly in injection. Once in the brain, these acetyl groups are removed to yield morphine, which causes the subjective effects of heroin. Thus, heroin may be thought of as a more rapidly acting form of morphine. Illicit morphine is rarely produced from codeine found in over-the-counter cough and pain medicines. This demethylation reaction is often performed using pyridine and hydrochloric acid.
The word analgesic derives from Greek an- (ἀν-, "without"), álgos (ἄλγος, "pain"), and -ikos (-ικος, forming adjectives). Such drugs were usually known as anodynes before the 20th century. Some novel and investigational analgesics include subtype-selective voltage-gated sodium channel blockers such as funapide and raxatrigine, as well as multimodal agents such as ralfinamide.. Audioanalgesia. Pain management. Patient-controlled analgesia. Pain in babies. Congenital analgesia (insensitivity to pain).
organicorganic chemistorganic chemical
For example, cholesterol-related compounds have opened ways to synthesize complex human hormones and their modified derivatives. Since the start of the 20th century, complexity of total syntheses has been increased to include molecules of high complexity such as lysergic acid and vitamin B 12. The discovery of petroleum and the development of the petrochemical industry spurred the development of organic chemistry.
Amines are formally derivatives of ammonia, wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines). Important amines include amino acids, biogenic amines, trimethylamine, and aniline; see for a list of amines. Inorganic derivatives of ammonia are also called amines, such as chloramine (NClH 2 ); see. The substituent -NH 2 is called an amino group.
In organic chemistry, functional groups are specific substituents or moieties within molecules that are responsible for the characteristic chemical reactions of those molecules. The same functional group will undergo the same or similar chemical reaction(s) regardless of the size of the molecule it is a part of. This allows for systematic prediction of chemical reactions and behavior of chemical compounds and design of chemical syntheses. Furthermore, the reactivity of a functional group can be modified by other functional groups nearby. In organic synthesis, functional group interconversion is one of the basic types of transformations.
It is an acetyl derivative of oxymorphone. It is related to other acetylated morphone derivatives, including 3,6-diacetyloxymorphone, 3,8,14-triacetyloxymorphone, 3,6,8,14-tetraacetyloxymorphone, noroxymorphone analogs of all or most of the above, and 3,6,14-triacetyloxymorphone, a derivative of oxymorphone whose structure-activity relationship suggests is 800% the potency of the parent drug versus 250% for 3,14-diacetyoxymorphone.
The drug has also been assessed at steroid hormone-associated carrier proteins, and shows very low binding to sex hormone-binding globulin (SHBG) but high affinity for corticosteroid-binding globulin (CBG) approximately equal to that of progesterone. 7α-Acetylthio-17α-hydroxyprogesterone, a related derivative of progesterone and also of 17α-hydroxyprogesterone, has been found to possess potent antimineralocorticoid activity similarly. Spironolactone is the derivative of this compound in which the acetyl group at the C17β position has been cyclized with the C17α hydroxyl group to form a spiro 21-carboxylic acid γ-lactone ring.
It is an acetyl derivative of oxymorphone and is an intermediate in the synthesis of several related drugs.
Norelgestromin (17β-deacetylnorgestimate, norgestrel 3-oxime)
Norelgestromin, also known as 17α-ethynyl-18-methyl-19-nortestosterone 3-oxime or as 17α-ethynyl-18-methylestr-4-en-17β-ol-3-one 3-oxime, is a synthetic estrane steroid and a derivative of testosterone. It is a racemic mixture of E and Z isomers, which have approximately the same activity. Norelgestromin is more specifically a derivative of norethisterone (17α-ethynyl-19-nortestosterone) and is a member of the gonane (18-methylestrane) subgroup of the 19-nortestosterone family of progestins. It is the C3 oxime derivative of levonorgestrel and the C17β deacetyl derivative of norgestimate and is also known as levonorgestrel 3-oxime and as 17β-deacetylnorgestimate.
CPA, also known as 1α,2α-methylene-6-chloro-17α-acetoxy-δ 6 -progesterone or as 1α,2α-methylene-6-chloro-17α-hydroxypregna-4,6-diene-3,20-dione acetate, is a synthetic pregnane steroid and an acetylated derivative of 17α-hydroxyprogesterone. It is structurally related to other 17α-hydroxyprogesterone derivatives such as chlormadinone acetate, hydroxyprogesterone caproate, medroxyprogesterone acetate, and megestrol acetate. Chemical syntheses of CPA have been published. The following is one such synthesis: CPA was first synthesized in 1961 by Rudolf Wiechert, a Schering employee, and together with Friedmund Neumann in Berlin, they filed for a patent for CPA as "progestational agent" in 1962.
In contrast, norelgestromin showed much weaker activity, indicating that the acetyl group of norgestimate is important for the activity. It was suggested by the researchers that norgestimate may be a promising lead compound for the development of new antibiotics.
acetyl CoAacetyl coenzyme Aacetyl-coenzyme A
CoA is acetylated to acetyl-CoA by the breakdown of carbohydrates through glycolysis and by the breakdown of fatty acids through β-oxidation. Acetyl-CoA then enters the citric acid cycle, where the acetyl group is oxidized to carbon dioxide and water, and the energy released captured in the form of 11 ATP and one GTP per acetyl group. Konrad Bloch and Feodor Lynen were awarded the 1964 Nobel Prize in Physiology and Medicine for their discoveries linking acetyl-CoA and fatty acid metabolism. Fritz Lipmann won the Nobel Prize in 1953 for his discovery of the cofactor coenzyme A.
aceticglacial acetic acidacetate
The name acetic acid derives from acetum, the Latin word for vinegar, and is related to the word acid itself. Glacial acetic acid is a name for water-free (anhydrous) acetic acid. Similar to the German name Eisessig (ice-vinegar), the name comes from the ice-like crystals that form slightly below room temperature at 16.6 C (the presence of 0.1% water lowers its melting point by 0.2 °C). A common symbol for acetic acid is AcOH, where Ac is the pseudoelement symbol representing the acetyl group −C(=O)−; the conjugate base, acetate, is thus represented as AcO − .
NATs transfer an acetyl group from acetyl-coenzyme A (Ac-CoA) to the α-amino group of the first amino acid residue of the protein. Different NATs are responsible for the acetylation of nascent protein N-terminal, and the acetylation was found to be irreversible so far. To date, six different NATs have been found in humans - NatA, NatB, NatC, NatD, NatE and NatF. Each of these different enzyme complexes is specific for different amino acids or amino acid sequences which is shown in the following table. '''Table 1.
tricarboxylic acid cycleKrebs cycleTCA cycle
The citric acid cycle begins with the transfer of a two-carbon acetyl group from acetyl-CoA to the four-carbon acceptor compound (oxaloacetate) to form a six-carbon compound (citrate). The citrate then goes through a series of chemical transformations, losing two carboxyl groups as CO 2 . The carbons lost as CO 2 originate from what was oxaloacetate, not directly from acetyl-CoA. The carbons donated by acetyl-CoA become part of the oxaloacetate carbon backbone after the first turn of the citric acid cycle. Loss of the acetyl-CoA-donated carbons as CO 2 requires several turns of the citric acid cycle.
Histone deacetylases (, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH 3 ) from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins.
Is or Tipp for the 2,4,6-triisopropylphenyl group (the former symbol is derived from the synonym isityl). Cp for the cyclopentadienyl group (Cp was the symbol for cassiopeium, a former name for lutetium). Cp* for the pentamethylcyclopentadienyl group. Ac for the acetyl group (Ac is also the symbol for the element actinium. However, actinium is almost never encountered in organic chemistry, so the use of Ac to represent the acetyl group never causes confusion). Bz for the benzoyl group; OBz is the benzoate group. Piv for the pivalyl (t-butylcarbonyl) group; OPiv is the pivalate group. Bt for the 1-benzotriazolyl group. Im for the 1-imidazolyl group.
Acyl-CoAs are acyl derivatives formed via fatty acid metabolism. Acetyl-CoA, the most common derivative, serves as an acyl donor in many biosynthetic transformations. Such acyl compounds are thioesters. Names of acyl groups of amino acids are formed by the replacement of the ending -ine by the ending -yl. For example, the acyl group of glycine is glycyl, and of lysine is lysyl. Names of acyl groups of ribonucleoside monophosphates such as AMP (5′-adenylic acid), GMP (5′-guanylic acid), CMP (5′-cytidylic acid), and UMP (5′-uridylic acid) are adenylyl, guanylyl, cytidylyl, and uridylyl respectively. In phospholipids, the acyl group of phosphatidic acid is called phosphatidyl-.
Ac 2 Oacetic anhydridesacetanhydride
Acetic anhydride is a versatile reagent for acetylations, the introduction of acetyl groups to organic substrates. In these conversions, acetic anhydride is viewed as a source of CH 3 CO +. Alcohols and amines are readily acetylated. For example, the reaction of acetic anhydride with ethanol yields ethyl acetate: : (CH 3 CO) 2 O + CH 3 CH 2 OH → CH 3 CO 2 CH 2 CH 3 + CH 3 COOH Often a base such as pyridine is added to function as catalyst. In specialized applications, Lewis acidic scandium salts have also proven effective catalysts. Aromatic rings are acetylated by acetic anhydride. Usually acid catalysts are used to accelerate the reaction.