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Kappa agonists, Opioids, Morphine, Opioid receptor ligands

Categories

Analgesics (2)
Drugs acting on the nervous system (2)
Ethers (2)
Euphoriants (2)
Mu-opioid agonists (2)
Natural opium alkaloids (2)
Opiates (2)
Opium (2)
Psychoactive drugs (2)
Pharmaceuticals (1)

morphine (64-31-3, 57-27-2)  
Morphia  ·  Morphine Sulfate  ·  MS Contin
Morphine is a pain medication of the opiate variety which is found naturally in a number of plants and animals. It acts directly on the central nervous system (CNS) to decrease the feeling of pain. It can be taken for both acute pain and chronic pain.

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Etorphine (14521-96-1)  
M99  ·  Ethorphine
Nalorphine hydrochloride (57-29-4)  
Nalorphine  ·  Allylnormorphine  ·  Lethidrone
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.
Bremazocine (83829-76-9, 75684-07-0, 79665-42-2)  
bremazocine hydrochloride, (2R)-isomer  ·  bremazocine hydrochloride, (+-)-isomer  ·  2-(1-hydroxy-cyclopropylmethyl)-5-ethyl-9,9-dimethyl-2'-hydroxy-6,7-benzomorphan
Bremazocine is a κ-opioid receptor agonist related to pentazocine. It has potent and long-lasting analgesic and diuretic effects. It has 200 times the activity of morphine, but appears to have no addictive properties and does not depress breathing.
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.
Naloxone hydrochloride (357-08-4)  
Naloxone  ·  Narcan  ·  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.
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.
CYCLAZOCINE (3572-80-3, 63903-61-7, 7346-09-0)  
Cyclazocine is a mixed opioid agonist/antagonist related to dezocine, pentazocine and phenazocine. This family of opioid drugs is called the benzomorphans or benzazocines. It is a KOR agonist and MOR partial agonist, and also has high affinity for the DOR.
Talwin (359-83-1, 55643-30-6)  
Pentazocine  ·  Pentazocine Hydrochloride  ·  Pentazocine Lactate
Pentazocine lactate (17146-95-1)  
Pentazocine  ·  Talwin  ·  Pentazocine Hydrochloride
pentazocine (7488-49-5, 359-83-1, 21820-34-8, 55643-30-6)  
Talwin  ·  Pentazocine Hydrochloride  ·  Pentazocine Lactate
Pentazocine, sold under the brand name Talwin among others, is a painkiller used to treat moderate to severe pain. It is believed to work by activating (agonizing) κ-opioid receptors (KOR) and blocking (antagonizing) μ-opioid receptors (MOR). As such it is called an opioid as it delivers its effects on pain by interacting with the opioid receptors.
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).
Nicomorphine (639-48-5)  
Vilan  ·  morphine dinicotinate  ·  bis(nicotinyl)morphine
Nicomorphine (Vilan, Subellan, Gevilan, MorZet) is the 3,6-dinicotinate ester of morphine. It is a strong opioid agonist analgesic two to three times as potent as morphine with a side effect profile similar to that of dihydromorphine, morphine, and diamorphine. Nicomorphine was patented as Vilan by Lannacher Heilmittel G.m.b.H.
ENADOLINE (124378-77-4)  
Enadoline is a drug which acts as a highly selective κ-opioid agonist. In human studies, it produced visual distortions and feelings of dissociation, reminiscent of the effects of salvinorin A. It was studied as a potential analgesic, but abandoned because of the dose-limiting effects of dysphoria, which could be expected from a κ-opioid agonist.
Tramadol (123154-38-1, 27203-92-5)  
Ultram  ·  Tramal  ·  Tramadol Hydrochloride
Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually occurs within an hour. It is often combined with paracetamol (acetaminophen) as this is known to improve the efficacy of tramadol in relieving pain.
baclofen (62594-36-9, 1134-47-0)  
Lioresal  ·  Genpharm  ·  beta-(p-Chlorophenyl)-gamma-aminobutyric Acid
Baclofen, sold under the brand name Lioresal among others, is a medication used to treat spasticity. It is used as a central nervous system depressant and skeletal muscle relaxant although its effectiveness has not been clearly shown. It is also used in topical creams to help with pain.
Pravadoline (92623-83-1)  
Pravadoline (WIN 48,098) is an antiinflammatory and analgesic drug with an IC50 of 4.9 µM and a Ki of 2511 nM at CB1, related in structure to nonsteroidal anti-inflammtory drugs (NSAIDs) such as indometacin. It was developed in the 1980s as a new antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX). However, pravadoline was found to exhibit unexpectedly strong analgesic effects, which appeared at doses ten times smaller than the effective anti-inflammatory dose and so could not be explained by its action as a COX inhibitor.
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Kappa agonists
Opioids
Morphine
Opioid receptor ligands
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