Debrisoquine is a derivative of

guanidine Guanidine is the compound with the formula HNC(NH2)2. It is a colourless solid that dissolves in polar solvents. It is a strong base that is used in the production of plastics and explosives. It is found in urine predominantly in patients experi ...

. It 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, heart failure, kidney failure and myocardial infa ...

drug similar to

guanethidine Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptak ...

. Debrisoquine is frequently used for

phenotyping In genetics, the phenotype () is the set of observable characteristics or traits of an organism. The term covers the organism's morphology (physical form and structure), its developmental processes, its biochemical and physiological properties ...

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 ...

enzyme, a drug-metabolizing enzyme. Debrisoquine has been identified as a inhibitor of

TMPRSS2 Transmembrane protease, serine 2 is an enzyme that in humans is encoded by the ''TMPRSS2'' gene. It belongs to the TMPRSS family of proteins, whose members are transmembrane proteins which have a serine protease activity. The TMPRSS2 protein is ...

protease, which is involved in the

viral entry Viral entry is the earliest stage of infection in the viral life cycle, as the virus comes into contact with the host cell (biology), cell and introduces viral material into the cell. The major steps involved in viral entry are shown below. Desp ...

process of

SARS-CoV-2 Severe acute respiratory syndrome coronavirus 2 (SARS‑CoV‑2) is a strain of coronavirus that causes COVID-19, the respiratory illness responsible for the COVID-19 pandemic. The virus previously had the Novel coronavirus, provisional nam ...

. In a laboratory study, it showed antiviral activity by blocking the ability of the virus to enter human lung cells. The

part of the molecule also appears in guanoxan and

guanadrel Guanadrel is an antihypertensive agent. It is used in the form of its sulfate. Mechanism of action Guanadrel is a postganglionic adrenergic blocking agent. Uptake of guanadrel and storage in sympathetic neurons occurs via the norepinephrine pump; ...

. The 7-bromo analog of debrisoquine is called guanisoquin.

References

Adrenergic release inhibitors Antihypertensive agents Guanidines Tetrahydroisoquinolines {{antihypertensive-stub

See also

References