Nervous System Drugs

Adrafinil is a mild central nervous system stimulating drug typically employed to relieve excessive sleepiness and inattention in geriatric patients. It is also been used off-label to prevent fatigue or falling asleep for extended periods of time. Adrafinil does not currently have FDA approval and is thus unregulated in the United States. It was marketed in France and elsewhere in Europe under the trade name Olmifon until September 2011 when France's FDA equivalent reassessed the drug and withdrew marketing permission. Adrafinil is metabolized to [modafinil].

3-Methylmethcathinone, also known as 3-MMC and metaphedrone,is a designer drug from the substituted cathinone family. 3-MMC is closely related in structure to the more commonly known illicit drug mephedrone (4-MMC), and is illegal in most countries that have banned mephedrone as it is a structural isomer of it. However, 3-MMC has still appeared on the recreational drug market as an alternative to mephedrone, and was first identified being sold in Sweden in 2012.Unlike other legal highs 3-MMC was tested and characterized in large mammals,providing much more knowledge about it than is known about other synthetic cathinones. 3-MMC is a monoamine transporter substrate that potently inhibits norepinephrine uptake and displays more pronounced dopaminergic vs. serotonergic activity.

U-47700 is an opioid analgesic drug developed by a team at Upjohn in the 1970s. U-47700 was derived from an earlier opioid AH-7921. U-47700 is selective for the µ-opioid receptor with a Kd value of 5.3 nM compared to 910 nM for the κ-opioid receptor and has around 7.5 x the potency of morphine in animal models. U-47700 is the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. The team looked for the key moieties which gave the greatest activity. Upjohn posted over a dozen patents on related compounds, each optimizing one moiety until they discovered that U-47700 was the most active. U-47700 became the lead compound of selective kappa-opioid receptor ligands such as U-50488 (containing a single methylene spacer difference) and U-69,593, which share very similar structures. Its structure led to other chemists experimenting with it to see if rigid analogues would retain activity. Although not used medically, the selective kappa ligands are used in research.

2-Chlorodiazepam is a natural product found in Solanum tuberosum and Triticum aestivum with data available.

Nemorexant is an orexin receptor antagonist used to treat insomnia, chronic obstructive pulmonary disease and obstructive sleep apnea.