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.

Tertomotide (also known as GV1001) is a synthetic telomerase-specific peptide vaccine patented by Norsk Hydro Asa for the cancer treatment. The agent was initially developed as a cancer vaccine, for example, against pancreatic and prostate cancer. Telomerase, a reverse transcriptase normally repressed in healthy cells, is overexpressed in most cancer cells and plays a key role in cellular proliferation. Vaccination with Tertomotide may activate the immune system to mount a cytotoxic T-lymphocyte response against telomerase-expressing cells. Subsequently, in vivo studies have demonstrated the efficacy of Tertomotide in alleviating benign prostatic hyperplasia (BPH) symptoms by reducing the size of the prostate gland. The mechanism of action of Tertomotide has been proposed to be through its dual activity as a GnRH inhibitor and 5a-reductase inhibitor. The GnRH antagonist activity has been established by co-immunoprecipitation assay, demonstrating an interaction between Tertomotide and the GnRH receptor, which was abolished by pre-treatment with anti-GnRH receptor antibody.

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