Ligands organométalliques

Benazepril is a nonsteroidal anti-inflammatory drug that can be used to treat hypertension, heart failure and renal failure. It is an angiotensin-converting enzyme (ACE) inhibitor that blocks the conversion of angiotensin I to angiotensin II. This inhibition prevents the vasoconstrictive effects of this peptide, which are mediated through activation of the renin-angiotensin system.

Antagonist of D1-like dopamine receptor subtypes, D1 and D5 (Ki values 0.2 and 0.3 nM respectively). Agonist of serotonin receptors 5-HT1C and 5-HT2C (Ki values 6.3 nM and 9.3 nM respectively). Used to study the topography of D1 receptors in humans and animals. Reduces seizures in response to chemoconvulsants and has also been studied in other neurological disorders.

Natural neurotoxin

Apremilast is the commercial name of a phosphodiesterase-4 (PDE4) inhibitor developed to treat chronic inflammatory disorders. Similarly to thalidomide, the apremilast molecule carries a phthalimide ring, but it lacks however the glutarimide ring needed to bind to cereblon, specifically targeted by thalidomide. As a drug, apremilast is indicated for the treatment of psoriasis and psoriatic arthritis.

t-TUCB is a potent soluble epoxide hydrolase (sEH) inhibitor, which is a chemically synthesized compound. The mode of action of t-TUCB involves the inhibition of sEH, an enzyme responsible for the degradation of epoxyeicosatrienoic acids (EETs). By inhibiting sEH, t-TUCB effectively increases the levels of EETs, which are signaling molecules involved in numerous physiological processes, including inflammation, blood pressure regulation, and pain perception.

Inhibits RNAPII-mediated trasncription; immunosuppressant; anti-inflammatory

Agonist of hypothalamic neuropeptide LHRH

Mianserin is a tetracyclic antidepressant drug that has antihistaminic and hypnosedative properties. It is used to treat depression in adults and children, as well as other disorders such as chronic pain and irritable bowel syndrome. This drug’s mechanism of action is not fully understood but is said to block alpha-adrenergic, histamine H1 and serotonin receptors.

Methotrexate is a chemotherapeutic and immunosuppressive medication, which is a synthetic analog of folic acid. Its source is through chemical synthesis, mimicking the structure of dihydrofolate in order to exert its effects. Methotrexate acts primarily by inhibiting the enzyme dihydrofolate reductase (DHFR), leading to a decrease in tetrahydrofolate production. This disruption in folate metabolism results in the inhibition of DNA, RNA, and protein synthesis, which affects rapidly dividing cells.Methotrexate is employed broadly in clinical oncology as an antineoplastic agent, particularly in the treatment of leukemias, lymphomas, breast cancer, and osteosarcoma. Additionally, it serves as a cornerstone for managing autoimmune diseases such as rheumatoid arthritis and psoriasis, where it helps modulate the aberrant immune response. The dual role of Methotrexate in oncology and immunosuppression underscores its versatility and critical importance in therapeutic regimens. However, its use demands careful monitoring due to potential adverse effects on non-cancerous cells and organ systems, necessitating precise dosage management and patient evaluation.

Naftopidil is an alpha adrenergic antagonist drug that is used to treat urinary symptoms and conditions related to benign prostatic hypertrophy. This drug works to relax smooth muscles by inhibiting alpha adrenergic receptors, thus allowing an improvement in urine flow.

A potent inhibitor of EGFR with sensitizing and T790M resistance mutations, selective over the wild-type form of the receptor. Causes tumour regression in EGFR mutant T790M transgenic and xenograft models in vivo.

Serotonin (5-HT7) receptor antagonist; anti-psychotic

Smoothened agonist and activator of the Hedgehog signalling pathway with EC50 of 3 nM. SAG binds to the Smoothened heptahelical bundle and antagonises effects of the Smoothened antagonist cyclopamine. In previous studies, SAG activated neurogenesis and neuronal survival in cell and animal models as well as improved cell differentiation of human induced pluripotent cells into the neuronal lineage.

Vanilloid receptor 1 antagonist

Acetylcholinesterase inhibitor; therapy for Alzheimer's disease

H1-receptor antagonist