Ajmalicine, also known as δ-yohimbine or raubasine, is an

antihypertensive Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Evidence suggests that ...

drug A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via inhal ...

used in the treatment of high

blood pressure Blood pressure (BP) is the pressure of circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressur ...

. It has been marketed under numerous brand names including Card-Lamuran, Circolene, Cristanyl, Duxil, Duxor, Hydroxysarpon, Iskedyl, Isosarpan, Isquebral, Lamuran, Melanex, Raunatin, Saltucin Co, Salvalion, and Sarpan. It is an

alkaloid Alkaloids are a class of basic BASIC (Beginners' All-purpose Symbolic Instruction Code) is a family of general-purpose, high-level programming languages designed for ease of use. The original version was created by John G. Kemeny and Th ...

found naturally in various plants such as ''

Rauvolfia ''Rauvolfia'' (sometimes spelled ''Rauwolfia'') is a genus of evergreen trees and shrubs, commonly known as devil peppers, in the family Apocynaceae. The genus is named to honor Leonhard Rauwolf. The genus can mainly be found in tropical regi ...

'' spp., '' Catharanthus roseus'', and ''

Mitragyna speciosa ''Mitragyna speciosa'' (commonly known as kratom, an herbal leaf from a tree of the Rubiaceae family, ) is a tropical evergreen tree in the coffee family native to Southeast Asia. It is indigenous to Thailand, Indonesia, Malaysia, Myanma ...

''. Ajmalicine is structurally related to yohimbine, rauwolscine, and other

yohimban Yohimban is a chemical compound. It is the base chemical structure of various alkaloids in the ''Rauvolfia'' and ''Corynanthe'' plant genera, including yohimbine, rauwolscine, corynanthine, ajmalicine, reserpine, deserpidine, and rescinnam ...

derivative In mathematics, the derivative of a function of a real variable measures the sensitivity to change of the function value (output value) with respect to a change in its argument (input value). Derivatives are a fundamental tool of calculus. ...

s. Like corynanthine, it acts as a α₁-adrenergic receptor antagonist with preferential actions over α₂-adrenergic receptors, underlying its hypotensive rather than hypertensive effects. Additionally, it is a very strong inhibitor of the

CYP2D6 Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the ''CYP2D6'' gene. ''CYP2D6'' is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra. CYP2 ...

liver enzyme, which is responsible for the breakdown of many drugs. Its binding affinity at this receptor is 3.30 nM.

References

Alkaloids found in Rauvolfia Alpha-1 blockers Antihypertensive agents Quinolizidine alkaloids Tryptamine alkaloids Indoloquinolizines Vinca alkaloids {{Antihypertensive-stub

See also

References