Aviptadil, a vasoactive intestinal polypeptide, is a vasodilator and lowers blood pressure if administered intravenously. In 2007, the orphan designation was granted by the European Commission for aviptadil for the treatment of sarcoidosis, a disease of unknown cause that affects many organs and tissues, most commonly the lungs. Sarcoidosis is characterized by specific microscopic lesions called granulomas. Aviptadil is able to influence the immune system that decreases the inflammatory processes seen in sarcoidosis by acting on the white blood cells (lymphocytes and monocytes) involved in the formation of the granulomas. In combination with phentolamine, the drug is used to treat erectile dysfunction. In addition, aviptadil has been studied in phase II clinical trials for patients with respiratory distress syndrome.

TAT-NR2B9C is a synthetic peptide fusion of the nine C-terminal residues of the NR2B subunit of the N-methyl-D-aspartate (NMDA) receptor and the cell membrane protein transduction domain of the HIV-1 tat protein. It is a postsynaptic density protein-95 (PSD95) inhibitor with neuroprotective properties. It is under development for the treatment of acute stroke and acute cerebral ischemia.

N-(2-Bromophenyl)-9-Methyl-9-Azabicyclo[3.3.1]Nonan-3-Amine (also known as AT-1001) is a high-affinity and highly selective ligand at α3β4 nicotinic cholinergic receptors (nAChRs) that was reported to decrease nicotine self-administration in rats. AT-1001 has a single-digit nanomolar binding affinity for the α3β4 nAChR and over 100-fold selectivity over the α4β2 nAChR and α7 nAChR in competition binding experiments. In electrophysiological experiments, AT-1001 had partial agonist activity at the α3β4 nAChR, evoking 35% of maximum ACh response, and at the same doses, produced desensitization of the ACh response, effectively acting as a functional antagonist at the α3β4 nAChR. Interestingly, AT-1001 also selectively decreased self-administration of cigarette smoke extract (CSE), an aqueous extract of cigarette smoke components, without altering natural food intake, when administered systemically to rats trained to self-administer CSE