Allyl compounds (1)
Cyclic compounds (1)
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.
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).
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.
oxilorphan hydrochloride, (9alpha,13alpha,14alpha)-isomer · oxilorphan, (14alpha)-(+-)-isomer · L-N-cyclopropylmethyl-3,14-dihydroxymorphinan
Oxilorphan (INN, USAN) (developmental code name L-BC-2605) is an opioid antagonist of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist, and has similar effects to naloxone and around the same potency as an MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR (with miosis, nausea, dizziness, and some euphoria observed) and can produce hallucinogenic/dissociative effects at sufficient doses, indicative of KOR activation.
nalodeine · N-allylnorcodeine · nalodeine hydrobromide, (5alpha,6alpha)-isomer
Nalodeine, also known more commonly as N-allylnorcodeine, is an opioid antagonist (specifically, an antagonist of the μ-opioid receptor) that was never marketed but is of notability in having been the first opioid antagonist to have been discovered. It was first reported in 1915, and this was followed by the clinical introduction of nalorphine (N-allylnormorphine) in 1954, naloxone (N-allyloxymorphone) in 1960, and naltrexone (N-methylcyclopropyloxymorphone) in 1963. Nalmefene (6-desoxy-6-methylene-naltrexone), another structurally related opioid antagonist derivative, was also subsequently introduced, in 1996.
Spiroxatrine is a drug which acts as a selective antagonist at both the 5-HT1A receptor and the α2C adrenergic receptor. It is an analog of spiperone and also has some dopamine antagonist effects.
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.
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.
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.
Spiroperidol · Spiroperone
Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class. It is licensed for clinical use in Japan as a treatment for schizophrenia. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl− channels (CaCCs), thus a potential target for therapy of cystic fibrosis.
QUINPIROLE (74196-92-2, 80373-22-4)
Quinpirole is a psychoactive drug and research chemical which acts as a selective D2 and D3 receptor agonist. It is used in scientific research. Quinpirole has been shown to increase locomotion and sniffing behavior in mice treated with it.
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.
Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.
Ro 48-8071 (161582-11-2)
Ro 48-8071hydrochloride · (4'-(6-allylmethylaminohexyloxy)-2'-fluorophenyl)-4-(4-bromophenyl)methanone fumarate · Ro-48-8071
Coramine · Coramin · Cordiamine
Nikethamide is a stimulant which mainly affects the respiratory cycle. Widely known by its former trade name of Coramine, it was used in the mid-twentieth century as a medical countermeasure against tranquilizer overdoses, before the advent of endotracheal intubation and positive-pressure lung expansion. It is no longer commonly considered to be of value for such purposes.
SKF 81297 · SK and F 81297 · SK and F-81297
SKF-81,297 is a synthetic drug of the benzazepine chemical class that acts as a selective dopamine D1/D5 receptor full agonist, and produces a characteristic stimulant-like pattern of anorexia, hyperactivity and self-administration in animals. This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958, but not with certain other D1 full agonists such as A-77,636, reflecting functional selectivity of D1 activation. Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D1-D2 receptor heteromers.
Nalorphine hydrochloride (57-29-4)
Nalorphine · Allylnormorphine · Lethidrone