Timelotem is a benzodiazepine derivative patented by Kali-Chemie Pharma G.m.b.H. as an anesthetic agent. In preclinical models, Timelotem shows atypical antipsychotic activity. Timelotem antagonizes DL-2-amino-5-phosphonovaleric acid (AP-5)-induced sniffing and the body turns in rats. Further, Timelotem antagonized amphetamine-induced stereotyped behavior in rats but was found less active than haloperidol in this test.

Delmetacin is a non-steroidal anti-inflammatory agent related to indomethacin. It has analgesic, antipyretic and anti-inflammatory properties.

Cyprazepam is a benzodiazepine tranquilizer, developed by Warner-Lambert Pharmaceutical Company in the 1960s. The combination of cyprazepam with pentaerythrityl tetranitrate was found advantageous for the treatment of angina pectoris.

Lergotrile is an ergot alkaloid clinically effective in the treatment of Parkinson’s disease. The in vivo dopaminergic effects of lergotrile are similar to those produced by the direct acting dopaminergic agonists apomorphine or L-DOPA. Like apomorphine or L-DOPA, lergotrile decreases prolactin secretion, produces stereotyped behavior in intact rats, and causes contralateral rotation in rats with uniIateral 6-hydroxydopamine lesions of substantia nigra. However, unlike apomorphine or L-DOPA, lergotrile does not activate dopamine sensitive adenylate cyclase in vitro. Side effects of lergotrile included exacerbation of hallucinations, dyskinesias, hypotension, and alterations in liver function tests. Although lergotrile, when added to levodopa, has a definite antiparkinsonian effect, the incidence of adverse effects, particularly hepatotoxicity, makes it unlikely that this ergot alkaloid will become widely available for the treatment of Parkinson’s disease.

LEIOPYRROLE is an antispasmodic agent.

LANIQUIDAR is a P-glycoprotein inhibitor. It was used in trials studying the treatment of breast cancer.

LASINAVIR, a hydroxyethylene derivative, is highly specific human immunodeficiency virus (HIV) protease inhibitor with an IC50 of 1 nM. Its clinical development was discontinued.

Nupafant (BB-960) is a potent platelet activating factor antagonist that is active both orally and intravenously. Nupafant was in phase I clinical trials in the UK for the treatment of ischemia-reperfusion injury, however this compound has since been suspended.

Mipitroban (previously known as UP 11677), a thromboxane A2 receptor antagonist that was investigated to treat thrombosis. However, further studies were apparently discontinued.

Nerispirdine, an acetylcholine release enhancer and a K+/Na+ use-dependent channel blocker, was in clinical development with sanofi-aventis for the treatment of multiple sclerosis. Nerispirdine is not proconvulsant. It can inhibit axonal K(+) channels and this mechanism may underlie the ability of the drug to enhance neuronal conduction. Nerispirdine can also inhibit neuronal Na(+) channels, a mechanism that may explain why nerispirdine lacks proconvulsant activity.