Sodelglitazar is an oral insulin sensitiser, a peroxisome proliferator-activated receptor (PPAR) pan agonist that was under development with GlaxoSmithKline for the treatment of hyperlipidaemia, type 2 diabetes mellitus and metabolic syndrome. Sodelglitazar exerts higher binding affinity for the delta subtype as compared to gamma and alpha subtypes. Sodelglitazar was being investigated in Phase II clinical trials for the treatment of T2DM and its complications, but this research has been discontinued.

Dabuzalgron is an orally active and selective alpha1A/1L-adrenoreceptor partial agonist, developed by Roche. In anesthetized micropigs and rabbits, dabuzalgron produced non-selective, dose-dependent increases in intraurethral and arterial blood pressures. In conscious micropigs, both agents produced dose-dependent increases in urethral tension. Dabuzalgron was investigated in a clinical study in women with stress urinary incontinence (SUI). It was demonstrated that 1.5 mg of the drug administered twice daily lead to a significantly lower mean weekly number of SUI episodes with little or no cardiovascular effect. Despite positive results, no development of the drug was reported by Roche.

Emapunil acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO). At the cellular level, the selective TSPO ligand XBD173 potentiated the amplitude and duration of GABA-mediated inhibitory postsynaptic currents in mouse medial prefrontal cortical neurons, which was prevented by finasteride. In animal and human trials, XBD173 produced rapid anxiolytic and anti-panic effects probably via newly synthesized neurosteroids, without producing sedation or withdrawal symptoms, and may represent a promising target for the development of fast-acting anxiolytics with a more favourable side-effect profile than benzodiazepines.

Tanaproget (WAY-166989) is a nonsteroidal progesterone receptor agonist. It has been in Phase-II clinical trials as an oral contraceptive. The compound demonstrated a positive preclinical pharmacological profile in the treatment of endometriosis. The level of progesterone receptors in breast tumours can be used to guide the selection of endocrine therapies for breast cancer patients. Radiolabeled analogues of tanaproget have diagnostic potential as PET imaging agents for breast cancer.

Osemozotan (also known as MKC-242) was developed as a selective 5-HT1A receptor agonist. Experiments on animal have shown that osemozotan improved most abnormal behaviors such as isolation rearing. Osemozotan was being investigated for the treatment of pain, aggressive behavior, anxiety, depression, obsessive-compulsive disorder, and drug dependence with methamphetamine and cocaine. However, all these studies were suspended. In the USA osemozotan participated in phase II clinical trial for the insomnia patients, however, the study was terminated because of the license agreement.

Naveglitazar is an oral dual peroxisome proliferator-activated receptor (PPAR) agonist, which was under development with Ligand Pharmaceuticals for the treatment of type 2 diabetes mellitus. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models and in the clinic. Naveglitazar had been in phase II clinical trials for the once-daily oral treatment of type 2 diabetes, however, the development was discontinued.

Mecloqualone is a quinazoline-class GABAergic and an analog of methaqualone. It acts as an agonist of the beta subtype of GABAa receptor and induces sedative, hypnotic and anxiolytic effects. Mecloqualone was marketed (mostly in france) under the names Nubrene and Casfen for the treatment of insomnia. Mecloqualone is no longer prescribed because of concerns about its potential for abuse and overdose. In the United States, it is registered as a Schedule-I non-narcotic controlled substance.

Pregnanediol is a chief steroid metabolite of progesterone that is biologically inactive and occurs as pregnanediol glucuronate in the urine. Pregnanediol has two hydroxyl groups, at 3-alpha and 20-alpha. A test can be done to measure the amount of pregnanediol in urine. The urine test offers an indirect way to measure progesterone levels in the body. It is a standard in the colorimetric determination of urinary pregnanediol in clinical laboratories.

Frakefamide is a tetrapeptide with an amide function at the C-terminus. The amino acid sequence of frakefamide is L-tyrosyl-D-alanyl-p-fluoro-L-phenylalanyl-Lphenylalaninamide. Hence, it contains both natural and unnatural R-amino acids. Frakefamide has shown interesting properties for use in acute and chronic pain treatment. It acts as a selective agonist on mu-opioid receptors and belongs to the dermorphin peptide family. It has been shown to be a potent peripherally acting analgesic in rats and humans. However, frakefamide had been found to have "unexpected results" in Phase II trials and AstraZeneca offered to hand the drug back.

LY-518674 is a highly potent and selective proliferator-activated receptor (PPAR)-alpha agonist. LY-518674 produced a much greater increase in serum high-density lipoprotein-cholesterol (HDL-c) than the known fibrate drugs. The increase in HDL-c was associated with de novo synthesis of apolipoprotein A-1. It was being developed for the treatment of dyslipidemias with atherogenic potential.