Spaglumic acid (NAAG) is the β-aspartyl isoform of N-Acetyl-l-aspartylglutamate (isospaglumic Acid is N-(N-Acetyl-l-α-aspartyl)-l-glutamic acid). In eye drops, spaglumic acid is either a magnesium or sodium salt of N-Acetyl-l-aspartylglutamate. Spaglumic acid is a mast cell stabilizer. Thus it is used in allergic conditions such as allergic conjunctivitis. Specifically spaglumic acid is approved in Portugal under the brand name Naabak and in Greece under the brand name Naaxia for use in patients with allergic conjunctivitis. Spaglumic Acid is a peptide neurotransmitter and the third-most-prevalent neurotransmitter in the mammalian nervous system. It is a weak activator of NMDA receptors and a highly selective agonist for mGlu3 receptors. Spaglumic Acid is neuroprotective under non-hydrolysing conditions in vivo.

Butoctamide (Butoctamide hydrogen succinate, BAHS), which is related to an organic compound naturally occurring in CSF, has been demonstrated to increase REM sleep in cats and young adults. BAHS was confirmed also to increase REM sleep in healthy aged subjects. The drug is marketed under the brand named Listomin S in Japan. It is effective against insomnia and other sleep disorders.

cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.

Clobenzorex is a central stimulant and sympathomimetic used as an anti-obesity drug; an n-substituted amphetamine, which is metabolized to amphethamine. Its actions are like those of dexamphetamine and has been used as a drug of abuse.

Glaziovine is a pro-aporphine alkaloid with neuropharmacological properties. Glaziovine is an alkaloid, originally isolated from Ocotea glaziovii (Lauraceae), belonging to the fairly small proaporphine family. In the early 1970's its pharmacology was explored extensively by a pharmaceutical company (Simes S.p.A., Milano), and was registered as a tranquilizer under the trademark Suavedol®. It is also reported to possess anti-ulcer properties in humans.

Benzoclidine (Oxylidin) exerts tranquilizing and hypotensive actions. It reduces the excitability of the central nervous system, enhances the effect of hypnotic drugs, analgesics and local anesthetics, has a moderate antihypertensive effect, reduces the excitability of the vasomotor centers, has anti-arrhythmic activity. Benzoclidine is marke indicated for the treatment of anxiety and depression of various origins (particularly mild expressed and associated with cerebrovascular insufficiency), neurosis, personality disorder, cyclothymia, hypertension with cerebral disorders, sinus tachycardia, paroxysmal tachycardia.

Oxilofrine is a sympathomimetic used to treat hypotensive states, with cardiac stimulatory effects similar to those of ephedrine. It has never been approved for use in the USA as a prescription drug or as a dietary supplement. Oxilofrine has been found (1) to act predominantly as a beta1 agonist increasing the speed and force of heart muscle contraction (inotropic effects), specifically, increasing left ventricular ejection fraction and stroke volume; (2) to increase blood pressure; (3) to have variable effects on heart rate; and (4) to potentially increase oxygen uptake by the lungs.

Budipine is an antiparkinsonian drug, which was developed by Byk Gulden (now Takeda) for the treatment of Parkinson's disease. The drug has multiple mechanisms of action: it was found to interfere with dopamine biosynthesis, mainly by inhibiting MAO-B enzyme and stimulating aromatic L-amino acid decarboxylase. Also the drug inhibits the dopamine re-uptake and has weak affinity to NMDA and muscarinic receptors. Budipine passes the blood-brain barrier, is metabolized by hydroxylation, and is excreted by both in urine and feces within 24 h.

Abecarnil (isopropyl 6-benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylate) is a nonselective mixed full agonist/partial agonist at GABA(A) receptor subtypes. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil has been studied in the treatment of anxiety disorders however its development has been discontinued.

Fenbutrazate is a prodrug of phenmetrazine, a psychostimulant for the treatment of obesity. Fenbutrazate acts as an agonist of monoamine transportes upon conversion to the active metabolite. The drug is no longer marketed due to its addictive profile.