Emopamil is a calcium channel blocker and a high-affinity

ligand In coordination chemistry, a ligand is an ion or molecule ( functional group) that binds to a central metal atom to form a coordination complex. The bonding with the metal generally involves formal donation of one or more of the ligand's elec ...

of human sterol

isomerase Isomerases are a general class of enzymes that convert a molecule from one isomer to another. Isomerases facilitate intramolecular rearrangements in which bonds are broken and formed. The general form of such a reaction is as follows: A–B � ...

Structure

Emopamil's structure consists of an organic

amino In chemistry, amines (, ) are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent ...

compound, nitrile compound and a member of two benzene rings.

Applications

Emopamil also known as EMP is a

phenylalkylamine Substituted phenethylamines (or simply phenethylamines) are a chemical class of organic compounds that are based upon the phenethylamine structure; the class is composed of all the derivative compounds of phenethylamine which can be formed by ...

and inhibitor of

5-hydroxytryptamine Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...

5-HT2 receptors. EMP includes a chiral quaternary carbon center, and research has indicated that its optical isomers have different biological effects. It interacts in an extracellular site of the

nerve cell A neuron, neurone, or nerve cell is an electrically excitable cell that communicates with other cells via specialized connections called synapses. The neuron is the main component of nervous tissue in all animals except sponges and placozoa. No ...

to inhibit calcium channel responses while other phenylalkylamines act at an intracellular site. The interaction site of emopamil suggests to its greater neuroprotective efficacy in research related to

ischaemia Ischemia American and British English spelling differences#ae and oe, or ischaemia is a restriction in blood supply to any tissue (biology), tissue, Skeletal muscle, muscle group, or Organ (biology), organ of the body, causing a shortage of oxyg ...

.Keith RA, Mangano TJ, DeFeo PA, Ernst GE, Warawa EJ. Differential inhibition of neuronal calcium entry and HD-aspartate release by the quaternary derivatives of verapamil and emopamil. Br J Pharmacol. 1994 Oct;113(2):379-84. doi: 10.1111/j.1476-5381.1994.tb16999.x. PMID: 7834187; PMCID: PMC1510140.

References

{{biochem-stub Calcium channel blockers Nitriles Amines Isopropyl compounds

Structure

Applications

See also

References