As a narcotic antagonist similar in action to naloxone, DIPRENORPHINE is used to remobilize animals after analgesia by super-potent opioid analgesics such as etorphine and carfentanil. It is not used in humans. Diprenorphine binds approximately equally to the three subtypes of opioid receptors (mu, delta, and kappa) and antagonizes them. This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene. The therapeutic efficacy of many other compounds can be decreased when used in combination with Diprenorphine (54 compounds mentioned on www.drugbank.ca).

PAI-749 is a small molecule inhibitor of PAI-1 with proven antithrombotic efficacy in several preclinical models. PAI-1 inactivation by PAI-749 using purified components can result from a dual mechanism of action. First, PAI-749 binds directly to PAI-1, blocks PAI-1 from accessing the active site of tPA, and abrogates formation of the SDS-stable tPA/PAI-1 complex. Second, binding of PAI-749 to PAI-1 renders PAI-1 vulnerable to plasmin-mediated proteolytic degradation. Despite its efficacy in a purified human system and in preclinical models of thrombosis, the ex vivo clinical study suggests that PAI-749 does not affect thrombus formation or fibrinolysis in a range of established human plasma and whole blood-based systems.

Decimemide is a spasmolytic and anticonvulsant derivative of benzamide, developed by the Hungarian E.G.Y.R Gyogyszervegyeszeti Gyar. The compound is claimed to effectively inhibit convulsion caused by chemoconvulsants or electric shock and to have a strong antiepileptic effect without showing any neurodepressant character.

Dacopafant (R-enantiomer RP 55778, racemate RP 48740) is an antagonist fo a platelet-activating factor and an inhibitor of TNH-alpha synthesis. It was developed by Rhone-Poulenc Rorer (France, now Aventis). In vitro, treatment of HIV-1 infected monocyte-derived macrophages with dacopafant resulted in a significant decrease in TNF-alpha levels and viral production. RP 48740 inhibited [3H]PAF platelet binding with IC50 of 2.3 uM and antagonized PAF-induced platelet activation with IC50 of 16 uM. In a clinical trial on human volunteers, RP 48740 was well tolerated and inhibited ex vivo platelet aggregation by as much as 79% 6 hr after administration.

Pleuromulin (pleuromulitin) is a natural antibiotic isolated from Basidiomycete Pleurotus. Pleuromulitin exhibits activity mainly against gram-positive bacteria including S. aureus, Klebasiella pneumoniae and Bacillus Subtilis. Pleuromulin is an organic compound which is not reported to be used in as a drug however its derivatives have been used in treatment of infections. The first pleuromulitin that was approved in 1979 for use in veterinary medicine was semi-synthetic derivative tiamulin. Semisynthetic pleuromutilin retapamulin (ALTABAX, GlaxoSmithKline) was the first approved for topical use in humans in 2007. Another derivative of pleuromulin, Lefamulin has been successfully tested in phase 1 clinical trial for systemic use in patients (Nabriva Therapeutics AG).

Pinolcaine is 10-methyl-2-substituted piperidine. Pinolcaine is a local anesthetic.

Picoplatin is a sterically hindered platinum (II) complex with antineoplastic properties developed for the treatment of cis-platin-resistant cancer. Picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. However, in Phase III trials, picoplatin failed to meet its primary endpoint for advanced cell lung cancer. It remains in development for other cancers.

Drinabant is a selective CB1 receptor antagonist under investigation varyingly as a treatment for obesity, schizophrenia, Alzheimer's disease, Parkinson's disease, and nicotine dependence. Drinabant may be useful to treat the cognitive deficits in schizophrenia and as a co-treatment with currently available antipsychotics. Coadministration of olanzapine and drinabant attenuated body weight gain, diminishing the enhanced food intake while maintaining increased energy expenditure and decreased motility. Sanofi has outlicensed global development and commercialization rights to drinabant to Opiant Pharmaceuticals, which said it plans to start developing the acute cannabinoid overdose (ACO) candidate in the 2019 year. Opiant said drinabant will be developed as an injectable for administration in an emergency department setting.

The natural tetrapeptide acetyl-N-Ser-Asp-Lys-Pro (AcSDKP also known as Goralatide) is generated from the N-terminus of thymosin-β4 through enzymatic cleavage by prolyl oligopeptidase (POP). AcSDKP regulation of proliferation of different cells is implicated in hematopoiesis and angiogenesis. This tetrapeptide present in almost all cells was recently detected at elevated concentrations in neoplastic diseases. However, previously reported in vitro and in vivo studies indicate that AcSDKP does not contribute to the pathogenesis of cancers. AcSDKP was in the phase II clinical trial for development of a new non-radioactive test for measuring glomerular filtration rate in patient with Chronic Kidney Disease. In addition, using mice models was concluded ,that AcSDKP might be an oral antifibrotic peptide drug that would be relevant to combating fibroproliferative kidney diseases such as diabetic nephropathy.

Alozafone is an anticonvulsant (CNS depressant).