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Kappa agonists, Local anesthetics

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Analgesics (1)
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meperidine (57-42-1)  
Demerol  ·  Dolin  ·  Pethidine
Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a synthetic opioid pain medication of the phenylpiperidine class. Synthesized in 1939 as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized by Otto Schaumann while working for IG Farben, Germany. Pethidine is the prototype of a large family of analgesics including the pethidine 4-phenylpiperidines (piminodine, anileridine and others), the prodines (alphaprodine, MPPP, etc.), bemidones (ketobemidone, etc.) and others more distant, including diphenoxylate and analogues.

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propofol (2078-54-8)  
Diprivan  ·  ICI 35,868  ·  Pisa Brand of Propofol
Propofol, marketed as Diprivan among others, is a short-acting medication that results in a decreased level of consciousness and lack of memory for events. Its uses include the starting and maintenance of general anesthesia, sedation for mechanically ventilated adults, and procedural sedation. It is also used for status epilepticus if other medications have not worked.
(+/-)-Epibatidine (140111-52-0)  
Epibatidine is a putative alkaloid that is secreted by the Ecuadoran frog Epipedobates anthonyi. It was discovered by John W. Daly in 1974, but its structure was not fully elucidated until 1992.
isoflurane (26675-46-7)  
Isoflurane, sold under the trade name Forane among others, is a general anesthetic. It can be used to start or maintain anesthesia. Often another medication, however, is used to start anesthesia due to airway irritation with isoflurane.
Allopregnanolone (128-20-1, 516-55-2)  
Pregnanolone  ·  3 alpha, 5 beta-Tetrahydroprogesterone  ·  Pregnanolone, (3beta, 5beta)-isomer
clonidine (4205-90-7)  
Catapres  ·  Clonidine Hydrochloride  ·  Dixarit
Clonidine (trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist that has been in clinical use since 1966.
Pregnanolone (128-20-1)  
Pregnanolone, also known as eltanolone (INN), as well as 3α,5β-tetrahydroprogesterone (3α,5β-THP) or 3α-hydroxy-5β-pregnan-20-one, is an endogenous neurosteroid that is biosynthesized from progesterone. It is a positive allosteric modulator of the GABAA receptor, as well as a negative allosteric modulator of the glycine receptor, and is known to have sedative, anxiolytic, anesthetic, and anticonvulsant effects. It was investigated for clinical use as a general anesthetic, but produced unwanted side effects such as convulsions on occasion, and for this reason was never marketed.
SPIRADOLINE (87151-85-7)  
Spiradoline (U-62066) is a drug which acts as a highly selective κ-opioid agonist. It has analgesic, diuretic and antitussive effects, and produces subjective effects in animals similar to those of ketazocine and alazocine. The main effect in humans is sedation, along with analgesic and diuretic effects, but significant side effects such as dysphoria and hallucinations have stopped it from being used clinically.
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.
Nalorphine hydrochloride (57-29-4)  
Nalorphine  ·  Allylnormorphine  ·  Lethidrone
dibucaine (61-12-1, 85-79-0)  
Nupercaine  ·  Nupercainal  ·  Cinchocaine
Cinchocaine (INN/BAN) or dibucaine (USAN) is an amide local anesthetic. Among the most potent and toxic of the long-acting local anesthetics, current use of cinchocaine is generally restricted to spinal and topical anesthesia. It is sold under the brand names Cincain, Nupercainal, Nupercaine and Sovcaine.
Etorphine (14521-96-1)  
M99  ·  Ethorphine
CLONIDINE HYDROCHLORIDE (4205-91-8)  
Clonidine  ·  Catapres  ·  Dixarit
Clonidine (trade names Catapres, Kapvay, Nexiclon, Clophelin, and others) is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, anxiety disorders, tic disorders, withdrawal (from either alcohol, opioids, or smoking), migraine, menopausal flushing, diarrhea, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist and imidazoline receptor agonist that has been in clinical use since 1966.
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.
prilocaine (721-50-6)  
Citanest  ·  Prilocaine Hydrochloride  ·  Propitocaine
Prilocaine () is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils Löfgren. In its injectable form (trade name Citanest), it is often used in dentistry. It is also often combined with lidocaine as a topical preparation for dermal anesthesia (lidocaine/prilocaine or EMLA), for treatment of conditions like paresthesia.
Midazolam maleate (59467-94-6)  
Versed  ·  Midazolam  ·  Midazolam Hydrochloride
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.
midazolam (59467-70-8)  
Versed  ·  Midazolam Hydrochloride  ·  Dormicum
Midazolam, marketed under the trade name Versed, among others, is a medication used for anesthesia, procedural sedation, trouble sleeping, and severe agitation. It works by inducing sleepiness, decreasing anxiety, and causing a loss of ability to create new memories. It is also useful for the treatment of seizures.
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Kappa agonists
Local anesthetics
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