Medicinal plants, also called medicinal herbs, have been discovered and used in traditional medicine practices since prehistoric times. Plants synthesise hundreds of chemical compounds for functions including defence against insects, fungi, diseases, and herbivorous mammals. Numerous phytochemicals with potential or established biological activity have been identified. However, since a single plant contains widely diverse phytochemicals, the effects of using a whole plant as medicine are uncertain. Further, the phytochemical content and pharmacological actions, if any, of many plants having medicinal potential remain unassessed by rigorous scientific research to define efficacy and safety.
Tiagabine is an anticonvulsant medication produced by Cephalon that is used in the treatment of epilepsy. The drug is also used off-label in the treatment of anxiety disorders and panic disorder.
Butriptyline, sold under the brand name Evadyne among others, is a tricyclic antidepressant (TCA) that has been used in the United Kingdom and several other European countries for the treatment of depression but appears to no longer be marketed. Along with trimipramine, iprindole, and amoxapine, it has been described as an "atypical" or "second-generation" TCA due to its relatively late introduction and atypical pharmacology. It was very little-used compared to other TCAs, with the number of prescriptions dispensed only in the thousands.
Phenacemide, also known as phenylacetylurea, is an anticonvulsant of the ureide (acetylurea) class. It is a congener and ring-opened analogue of phenytoin, and is structurally related to the barbiturates and to other hydantoins. Phenacemide was introduced in 1949 for the treatment of epilepsy, but was eventually withdrawn due to toxicity.
Melitracen is a tricyclic antidepressant (TCA), for the treatment of depression and anxiety. In addition to single drug preparations, it is also available as Deanxit, marketed by Lundbeck, a combination product containing both melitracen and flupentixol.
The oxytocin receptor, also known as OXTR, is a protein which functions as receptor for the hormone and neurotransmitter oxytocin. In humans, the oxytocin receptor is encoded by the OXTR gene which has been localized to human chromosome 3p25.
Isoaminile is an antitussive used under the trade-name Peracon.
The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it.
Arylcyclohexylamines, also known as arylcyclohexamines or arylcyclohexanamines, are a chemical class of pharmaceutical, designer, and experimental drugs.
Cyclorphan is an opioid analgesic of the morphinan family that was never marketed. It acts as a μ-opioid receptor (MOR) weak partial agonist or antagonist, κ-opioid receptor (KOR) full agonist, and, to a much lesser extent, δ-opioid receptor (DOR) agonist. The drug was first synthesized in 1964 by scientists at Research Corporation. In clinical trials, it had relatively long duration, good absorption, and provided strong pain relief but produced psychotomimetic effects via KOR activation, so its development was not continued.
Noxiptiline, also known as noxiptyline and dibenzoxine, is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1970s for the treatment of depression. It has imipramine-like effects, acting as a serotonin and norepinephrine reuptake inhibitor, among other properties. Of the TCAs, noxiptiline has been described as one of the most effective, rivaling amitriptyline in clinical efficacy.
Imipraminoxide, or imipramine N-oxide, is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1960s for the treatment of depression.
Glicaramide (SQ-65993) is an orally bioavailable anti-diabetic medication. It has a similar potency as glibenclamide (glyburide) in the class of medication known as sulfonylureas. Its structure is similar since it has a cyclic acyl group which replaces the latter's 2-methoxy-5-chlorobenzyl. Same as glibenclamide, it is classified as a second-generation sulfonylurea. It may have more pronounced extra-pancreatic effects than glibenclamide or tolbutamide.
PD-0298029 is a drug which acts as a selective antagonist for the muscarinic acetylcholine receptor M4. It was developed for the treatment of Parkinson's disease, but poor bioavailability and rapid metabolism in animal studies have meant its use is largely limited to in vitro research into the M4 and other muscarinic receptors.
Substituted tryptamines, or serotonin analogues, are organic compounds which may be thought of as being derived from tryptamine itself. The molecular structures of all tryptamines contain an indole ring, joined to an amino (NH2) group via an ethyl (−CH2–CH2−) sidechain. In substituted tryptamines, the indole ring, sidechain, and/or amino group are modified by substituting another group for one of the hydrogen (H) atoms.
Tonazocine (WIN-42,156) is an opioid analgesic of the benzomorphan family which made it to phase II clinical trials for the treatment of postoperative pain, but development was apparently ceased and ultimately it was never marketed. Tonazocine is a partial agonist at both the mu-opioid and delta-opioid receptors, but acting more like an antagonist at the former and more like an agonist at the latter. It lacks most of the side effects of other opioids such as adverse effects on the cardiovascular system and respiratory depression, but it can cause sedation, and in some patients it may induce hallucinations.
Plomestane is a steroidal, irreversible aromatase inhibitor which was under development by Marion Merrell Dow/Hoechst Marion Russell as an antineoplastic agent for the treatment of breast cancer. It was found to be effective in preclinical studies and was also found to produce few adverse effects in human clinical trials, significantly reducing estrogen levels with a single administration. However, development of the drug for clinical use was halted due to "technical issues" and it was never marketed.
Ralfinamide (INN) is a multimodal drug which is under investigation by Newron Pharmaceuticals for the treatment of neuropathic pain and other pain conditions such as post-operative dental pain.
Allyltestosterone, or 17α-allyltestosterone, also known as 17α-allylandrost-4-en-17β-ol-3-one, is a steroid derived from testosterone that was first synthesized in 1936 and was never marketed. Along with propyltestosterone (topterone), it has been patented as a topical antiandrogen and hair growth inhibitor. Allyltestosterone is the parent structure of two marketed 19-nortestosterone progestins, allylestrenol and altrenogest. These progestins are unique among testosterone derivatives in that they appear to be associated with few or no androgenic effects.
Pinoxepin is an antipsychotic of the tricyclic group with a dibenzoxepin ring system which was developed in the 1960s but was never marketed. It was found in clinical trials to have effectiveness in the treatment of schizophrenia similar to that of chlorpromazine and thioridazine. The drug has marked sedative effects but causes relatively mild extrapyramidal symptoms.
↑ Johnson O, Jones DW, Nagarajan K, Bhadbhade MM, Venkatesan K (1992). "X-ray crystal structure analysis of nitroxazepine: 10-(3-dimethylaminopropyl)-2-nitro-10,11-dihydrodibenz [b,f][l,4]oxazepin-11-one". Journal of Chemical Crystallography. 22 (5): 579–583. doi:10.1007/BF01161343. S2CID96236391.
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