Diperodon is one of several phenylurethane derivatives of dialkyl amino alcohols which have demonstrated significant local anaesthetic activity.

Cyclopropane is a cycloalkane, consisting of three carbon atoms, linked to each other to form a ring. Cyclopropane was used as an anesthetic gas since the 1920s, due to being non-irritant, giving rapid induction, excellent relaxation, quiet respiration, and speedy recovery. However, the prolonged administration of cyclopropane may induce a reaction known as "cyclopropane shock", which manifests in a sudden decrease in blood pressure, potentially leading to cardiac dysrhythmia. Because of the toxicity and extreme flammability, cyclopropane was used only for the induction of anesthesia and was gradually superseded by more safe anesthetics. Cyclopropane works by blocking NMDA and AMPA receptors and activating K2P channels, kainate ion channels and glycine receptors at clinical concentrations.

Sodium thiopental (also known as Sodium Pentothal, thiopental) was discovered in 1930s by investigators working for Abbott Laboratories. Thiopental sodium was used for the induction of general anesthesia and is used as an adjunct to provide hypnosis during balanced anesthesia with other anesthetic agents, including analgesics and muscle relaxants. Thiopental sodium was also used as an adjunct for control of convulsive disorders of various etiology, including those caused by local anesthetics. Finally, thiopental sodium had been used to reduce the intracranial pressure in patients with increased intracranial pressure, if controlled ventilation is provided. Nevertheless, these prescriptions of drug were discontinued. In addition, this drug was banned for use in US executions. Thiopental sodium acts through the CNS with particular activity in the mesencephalic reticular activating system. It was shown, that mechanism of action of sodium thiopental via GABAA receptor. Thiopental binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

Piperocaine (Metycaine) is a local anesthetic drug. It is an ester and primarily is a sodium channel blocker. Piperocaine can partially inhibit dopamine. It is known as a alpha-1-proteinase inhibitor. Used in the form of its hydrochloride as a local or spinal anesthetic and in dental anesthesia. Can cause toxic reactions. Piperocaine Hydrochloride is in the list of Bulk Drug Substances Nominated for Use in Compounding Under Section 503A, FDA Act. Piperocaine hydrochloride is a small, white odorless crystals or a white crystalline powder, stable in air, freely soluble in water, alcohol and chloroform.

Butacaine is a local anesthetic. It should not be used with people who have a history of allergies due to the possibility of anaphylactic shock.

Tricaine (MS-222, Tricaine-S), a water-soluble local anesthetic, is used commonly for sedation, immobilization, and anesthesia of poikilothermic animals and has been accepted as a common anesthetic for use in the cold-blooded animals. It has long been recognized as a valuable tool for the proper handling of these animals during manual spawning (fish stripping), weighing, measuring, marking, surgical operations, transport, photography, and research. Tricaine was developed by Merck as a sulfonated analog of benzocaine with high solubility in water. The main advantage of Tricaine is the short duration of action and rapid metabolism. There are many reports describing the use of Tricaine for anesthetizing poikilothermic animals because it is a safe agent for immersion anesthesia even though the other anesthetics such as ether, ethanol, thiopental, halothane, isoflurane, barbiturates also could be used. Amphibians could be anesthetized easily by immersion methods with Tricaine because the amphibian skin is extremely permeable and water is absorbed through the skin rather than ingested. Tricaine has been administered as an injectable agent also.

Amylocaine (trade name Stovaine) is a local anesthetic, that was widely used for spinal anesthesia in Caesarean section. The dose used would produce anesthesia for up to 1 h. Reports of the use of spinal analgesia for abdominal and perineal surgery in infants are found from several centers during the first half of the twentieth century. However, this agent often fails to provide good maternal sensory block and currently, Amylocaine has been replaced with new anesthetics.

Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.