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Opioid antagonists

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naloxone (465-65-6)  
Narcan  ·  Naloxone Hydrochloride  ·  Nalone
Naloxone, sold under the brandname Narcan among others, is a medication used to block the effects of opioids, especially in overdose. Naloxone may be combined within the same pill as an opioid to decrease the risk of misuse. When given intravenously, naloxone works within two minutes, and when injected into a muscle, it works within five minutes; it may also be sprayed into the nose.
naltrexone (16590-41-3, 16676-29-2)  
ReVia  ·  Trexan  ·  Naltrexone Hydrochloride
Naltrexone, sold under the brand names Revia and Vivitrol among others, is a medication primarily used to manage alcohol dependence and opioid dependence. In opioid dependence, it should not be started until people are detoxified. It is taken by mouth or by injection into a muscle.
buprenorphine (52485-79-7)  
Buprenex  ·  Buprenorphine Hydrochloride  ·  Subutex
Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain. It can be used under the tongue, by injection, as a skin patch, or as an implant. When used for opioid addiction it is recommended that a health care provider observe the person while they take the medication.
apigenin (520-36-5)  
Apigenin (4′,5,7-trihydroxyflavone), found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally occurring glycosides. It is a yellow crystalline solid that has been used to dye wool.
Nalorphine (62-67-9)  
Allylnormorphine  ·  Nalorphine Hydrochloride  ·  Lethidrone
Nalorphine (INN) (brand names Lethidrone, Nalline), also known as N-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence. It acts at two opioid receptors — the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (Ki = 1.6 nM; EC50 = 483 nM; Emax = 95%) where it exerts high-efficacy partial agonist/near-full agonist characteristics.
levallorphan (152-02-3)  
Lorfan  ·  Naloxiphan
Levallorphan (INN, BAN) (brand names Lorfan, Naloxifan, Naloxiphan), also known as levallorphan tartrate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote. It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR), and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine whilst simultaneously producing analgesia. Levallorphan was formerly widely used in general anesthesia, mainly to reverse the respiratory depression produced by opioid analgesics and barbiturates used for induction of surgical anaesthesia whilst maintaining a degree of analgesia (via KOR agonism).
Rimonabant (168273-06-1, 158681-13-1)  
Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) was an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States. Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was the first drug approved in that class.
lobeline (90-69-7)  
Smokeless  ·  Lobeline Sulfate  ·  Inibsa Brand of Lobelin Sulfate
Lobeline is an alkaloid found in a variety of plants, particularly those in the genus Lobelia, including Indian tobacco (Lobelia inflata), Devil's tobacco (Lobelia tupa), cardinal flower (Lobelia cardinalis), great lobelia (Lobelia siphilitica), Lobelia chinensis, and Hippobroma longiflora. In its pure form, it is a white amorphous powder which is freely soluble in water.
naringenin (480-41-1)  
naringenin-7-sulfate  ·  BE-14348A  ·  BE 14348A
Naringenin is a bitter, colourless flavanone, a type of flavonoid. It is the predominant flavanone in grapefruit, and is found in a variety of fruits and herbs.
Diprenorphine (14357-78-9)  
Revivon  ·  Diprenorphine Hydrochloride
Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high-affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) that is employed in veterinary medicine as an opioid antagonist. It is used to reverse the effects of super-potent opioid analgesics such as etorphine and carfentanil that are used for tranquilizing large animals. The drug is not approved for use in humans.
Cianidanol (154-23-4, 8001-48-7, 100786-01-4, 7295-85-4)  
Catechin  ·  Epicatechin  ·  Catechuic Acid
Catechin is a flavan-3-ol, a type of natural phenol and antioxidant. It is a plant secondary metabolite. It belongs to the group of flavan-3-ols (or simply flavanols), part of the chemical family of flavonoids.
(-)-Epicatechin (490-46-0)  
Catechin  ·  Epicatechin  ·  Catechuic Acid
Catechin is a flavan-3-ol, a type of natural phenol and antioxidant. It is a plant secondary metabolite. It belongs to the group of flavan-3-ols (or simply flavanols), part of the chemical family of flavonoids.
(R)-naringenin (480-41-1)  
naringenin  ·  naringenin-7-sulfate  ·  BE-14348A
Naringenin is a bitter, colourless flavanone, a type of flavonoid. It is the predominant flavanone in grapefruit, and is found in a variety of fruits and herbs.
(-)-Epicatechin gallate (1257-08-5)  
Epicatechin gallate (ECG) is a flavan-3-ol, a type of flavonoid, present in green tea. It is also reported in buckwheat and in grape. The tea component epicatechin gallate is being researched because in vitro experiments showed it can reverse methicillin resistance in bacteria like Staphylococcus aureus.
Hyperoside (482-36-0)  
hyperin  ·  quercetin-3-O-galactoside  ·  quercetin galactoside
Hyperoside is a chemical compound. It is the 3-O-galactoside of quercetin.
TAXIFOLIN (480-18-2)  
dihydroquercetin
Taxifolin is a flavanonol, a type of flavonoid.
AM251 (183232-66-8)  
AM 251  ·  N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide  ·  N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to SR141716A (rimonabant); both are biarylpyrazole cannabinoid receptor antagonists. In AM-251 the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group.
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