ALFETAMINE (aletamine) is an antidepressant and analgesic. The pharmacologic activity profile of aletamine closely resembles that of the tricyclic antidepressants imipramine and amitriptyline. Effects shared are antagonism of RO4-1284-induced ptosis and depressed exploratory behavior, depression of spontaneous motor activity, prolongation of hexobarbital hypnosis and anticonvulsant action in mice, hypotension and potentiation of norepinephrine pressor effects in dogs, antimuricidal effects, hypothermia in rats and local anesthesia in rabbits and guinea pigs. Aletamine differed from imipramine and amitriptyline as follows: (1) aletamine exerted no apparent central or peripheral anticholinergic effect as suggested by lack of influence on tremorine-induced tremors or salivation; (2) although aletamine was less potent on a milligram basis than imipramine and amitriptyline in preventing RO4-1284 depression, aletamine was more potent than imipramine in counteracting existing reserpine depression (ptosis, depressed exploratory behavior) in mice. Amitriptyline was inactive against reserpine depression. The pharmacologic effects of aletamine differ in several respects from those of d-amphetamine. The effects of aletamine on spontaneous motor activity, hexobarbital hypnosis and body temperature in rodents and on blood pressure in dogs are in opposite direction to those of amphetamine. In further contrast to amphetamine, grouping of mice has no influence on the toxicity of aletamine. Aletamine does not appear to be an inhibitor of monoamine oxidase in vivo since it does not enhance tryptamine-induced convulsions in rats.

Ciprefadol is an opioid analgesic drug. It binds with a high affinity to mu (Ki 4.2 nM) and kappa (Ki 2.5 nM) opioid receptors. In vivo, ciprefadol displays mixed antagonist/agonist activity in the mouse writhing and the rat tail heat tests: in low doses, the compound inhibits the analgesic effect of morphine, while at higher doses it displays analgesic effect. Chronic administration of ciprefadol to rhesus monkeys produced a marked physical dependence more severe than that of morphine, and its effect was consistent with what would be expected of a potent, long-lasting morphine-like agonist.

Lofemizole is a non-steroidal anti-inflammatory drug. Lofemizole has proved to possess an interesting antiphlogistic activity in both animals and humans, associated with a favorable gastric and systemic tolerability.

Telcagepant (MK-0974) is a calcitonin gene-related peptide receptor antagonist. Merck & Co was developing telcagepant for the treatment of pain. Telcagepant is an extremely potent CGRP antagonist with a Ki = 0.77 (0.07 nM). Telcagepant showed efficacy against acute migraines; however, different patient populations may show more beneficial effects with telcagepant versus triptans. In the acute treatment of migraine, Telcagepant was found to have equal potency to rizatriptan and zolmitriptan in two Phase III clinical trials. Merck & Co has now terminated development of the drug.

Bromadoline is a selective agonist of a μ-opioid receptor with potent analgesic activity developed by the Upjohn company in the 1970s for pain management.

Anilopam is an opioid analgesic of the benzazepine class. It is an opioid receptor agonist.

Indopine is indolylalkyl derivative patented by Irwin, Neisler and Co as potent analgesic.

Butopyrammonium is organic cationic compound.

Salethamide was developed as an anti-inflammatory agent to use as an analgesic. However, information about the further study of this compound is not available.

Xorphanol (also known as TR5379M) is a full κ-opioid receptor agonist and is a partial agonist at μ opioid receptor. Clinically, xorphanol was studied as an orally active analgesic that provided effective pain relief but showed low physical dependence liability. Further development of this drug was discontinued.