text: Even though μ-opioid receptor (MOR) targeting drugs have been used for a long time, not much is known about the structure-activity relationship and the ligand-receptor interactions on the basis of well-defined biological effects on receptor activation or inhibition. Also, the distinction in the receptor-ligand interaction patterns of agonists and antagonists is not known for sure. One theory states that the morphinans biological activity could be determined by the size of the N-substituents. For example, antagonists usually have larger substituents, such as allyl- or [https://pubchem.ncbi.nlm.nih.gov/compound/11029756 cyclopropyl methyl] at the morphinan nitrogen, while agonists generally contain a methyl group. On the other hand, agonist activity is also shown in ligands with larger groups at the morphinan nitrogen, and therefore this hypothesis is challenged.