Compounds capable of activating a neuronal heteromeric nicotinic acetylcholine receptor are provided and can be administered in the form of pharmaceutical compositions of the like. Methods for using the compounds for treating, preventing, or ameliorating respiratory depression and overdose induced by an opioid, or other cause of respiratory depression are also provided. Methods of inducing analgesia, anesthesia, or sedation in a subject, while simultaneously treating, preventing, or ameliorating respiratory depression and overdose induced by an opioid, or other cause of respiratory depression are also provided.