Ethallobarbital, also known as ethallymal and 5-allyl-5-ethylbarbituric acid, is an allyl-substituted barbiturate described as a sedative/hypnotic. It was first synthesized in 1927.
Minaxolone (CCI-12923) is a neuroactive steroid which was developed as a general anesthetic but was withdrawn before registration due to toxicity seen with long-term administration in rats, and hence was never marketed. It is a positive allosteric modulator of the GABAA receptor, as well as, less potently, a positive allosteric modulator of the glycine receptor.
Oxetorone, as oxetorone fumarate, is a serotonin antagonist, antihistamine, and alpha blocker used as an antimigraine drug. Association with hyperprolactinemia has been described and antidopaminergic actions are also suspected.
Alfadolone (INN), or alphadolone is a neuroactive steroid and general anesthetic. Along with alfaxolone, as alfadolone acetate, it is one of the components of the anesthetic drug mixture althesin.
Promestriene, also known as estradiol 3-propyl 17β-methyl diether, is a synthetic estrogen which is used topically in a 1% cream formulation for the treatment of vaginal atrophy in women. It is the 3-propyl and 17β-methyl diether of estradiol and does not appear to convert into estradiol in the body. Promestriene is minimally absorbed and appears to have negligible systemic estrogenic effect. The drug has been described as a tropic agent and antiseborrheic. It has not been found to be effective in the treatment of pattern hair loss or other conditions of cutaneous androgenization. Promestriene was first introduced in France in 1974 and has been marketed in 34 countries worldwide. It has been used in millions of women.
Methallenestril, also known as methallenoestril and as methallenestrol, as well as Horeau's acid, is a synthetic nonsteroidal estrogen and a derivative of allenolic acid and allenestrol that was formerly used to treat menstrual issues but is now no longer marketed. It is a seco-analogue of bisdehydrodoisynolic acid, and although methallenestril is potently estrogenic in rats, in humans it is only weakly so in comparison. Vallestril was a brand of methallenestril issued by G. D. Searle & Company in the 1950s. Methallenestril is taken by mouth. By the oral route, a dose of 25 mg methallenestril is approximately equivalent to 1 mg diethylstilbestrol, 4 mg dienestrol, 20 mg hexestrol, 25 mg estrone, 2.5 mg conjugated estrogens, and 0.05 mg ethinylestradiol.
Ibazocine is an opioid analgesic which was never marketed.
Diacetylnalorphine (BAN), also known as O3,O6-diacetyl-N-allyl-normorphine, is an opioid drug described as an analgesic and antidote which was never marketed. It is the 3,6-diacetyl ester of nalorphine, and therefore the heroin analogue of nalorphine. Diacetylnalorphine may behave as a prodrug to nalorphine, similarly to the cases of heroin (diacetylmorphine) to morphine and diacetyldihydromorphine to dihydromorphine.
Octotiamine (INN, JAN; Gerostop, Neuvita, Neuvitan), also known as thioctothiamine, is an analogue of vitamin B1 which is used in Japan and Finland.
Morforex, also referable to as N-morpholinoethylamphetamine, is an anorectic which was never marketed.
Picilorex is an anorectic which is no longer marketed. It is a monoamine reuptake inhibitor, a stimulant as well as a derivate of Pyrrolidine.
Acridorex is an amphetamine which was investigated as an anorectic but does not appear to have ever been marketed.
Oxifentorex (INN) is an amphetamine described as an anorectic which does not appear to have ever been marketed.
Fenisorex is an amphetamine-like anorectic drug which does not appear to have ever been marketed.
Flucetorex (INN) is an amphetamine. It was investigated as an anorectic, but does not appear to have been marketed. It is related to fenfluramine.
Metaglycodol (INN) is a drug described as a tranquilizer which was never marketed.
Perafensine (INN) is a drug which was investigated as an antidepressant but was never marketed. It has been reported to antagonize the effects of reserpine and to inhibit the reuptake of norepinephrine ; whether it also affects the reuptake of serotonin or dopamine is unclear.
Hydromadinone (INN), also known as 6α-chloro-17α-hydroxyprogesterone, is a steroidal progestin of the 17α-hydroxyprogesterone group which was patented in 1967 but was never marketed. The C17α acetate ester of hydromadinone, hydromadinone acetate, also exists, but similarly was never marketed.
Methestrol or methoestrol, also known as promethestrol or promethoestrol or as dimethylhexestrol, is a synthetic nonsteroidal estrogen of the stilbestrol group related to diethylstilbestrol which is no longer marketed.
Cioteronel is a nonsteroidal antiandrogen (NSAA) that was never marketed. It was under development between 1989 and 2001 for the topical treatment of androgenetic alopecia, and acne and for the oral treatment of benign prostatic hyperplasia; it reached phase III clinical trials for acne and phase II studies for androgenetic alopecia, but was ultimately discontinued due to poor efficacy.
