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Debrisoquine

From Wikipedia, the free encyclopedia

Debrisoquine^[1]
Names

Preferred IUPAC name 3,4-Dihydroisoquinoline-2(1H)-carboximidamide
Identifiers
CAS Number	1131-64-2^Y
3D model (JSmol)	Interactive image
ChEBI	CHEBI:34665^Y
ChEMBL	ChEMBL169901^Y
ChemSpider	2860^Y
DrugBank	DB04840^Y
ECHA InfoCard	100.013.155
KEGG	C13650^Y
MeSH	Debrisoquine
PubChem CID	2966
UNII	X31CDK040E^Y
CompTox Dashboard(EPA)	DTXSID7022885
InChI InChI=1S/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12)^Y Key: JWPGJSVJDAJRLW-UHFFFAOYSA-N^Y InChI=1/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12) Key: JWPGJSVJDAJRLW-UHFFFAOYAE
SMILES [N@H]=C(N)N2Cc1c(cccc1)CC2
Properties
Chemical formula	C₁₀H₁₃N₃
Molar mass	175.23032
Pharmacology
ATC code	C02CC04 (WHO)
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). Y verify (what is ^YN ?) Infobox references

Chemical compound

Debrisoquine is a derivative ofguanidine. It is anantihypertensive drug similar toguanethidine. Debrisoquine is frequently used forphenotyping theCYP2D6 enzyme, a drug-metabolizing enzyme.^[2]

Debrisoquine has been identified as a inhibitor ofTMPRSS2 protease, which is involved in theviral entry process ofSARS-CoV-2. In a laboratory study, it showed antiviral activity by blocking the ability of the virus to enter human lung cells.^[3]

Theguanidine part of the molecule also appears inguanoxan andguanadrel.^{[citation needed]} The 7-bromo analog of debrisoquine is calledguanisoquin.^{[citation needed]}

References

[edit]

^Debrisoquine – Compound Summary,PubChem.
^Fuhr, U.; Jetter, A.; Kirchheiner, J. (2007). "Appropriate Phenotyping Procedures for Drug Metabolizing Enzymes and Transporters in Humans and Their Simultaneous Use in the "Cocktail" Approach".Clinical Pharmacology & Therapeutics.81 (2):270–283.doi:10.1038/sj.clpt.6100050.PMID 17259951.
^Peiffer AL, Garlick JM, Wu Y, Wotring JW, Arora S, Harmata AS, Bochar DA, Stephenson CJ, Soellner MB, Sexton JZ, Brooks CL, Mapp AK (June 2023)."TMPRSS2 Inhibitor Discovery Facilitated through an In Silico and Biochemical Screening Platform".ACS Medicinal Chemistry Letters.14 (6):860–866.doi:10.1021/acsmedchemlett.3c00035.PMC 10237299.PMID 37284689.

Sympatholytic (and closely related)antihypertensives (C02)

Sympatholytics
(antagonizeα-adrenergic
vasoconstriction)

Central

α₂-Adrenergic receptor agonists	Clonidine Guanabenz Guanfacine Guanoxabenz Methyldopa^# Tiamenidine^‡
Adrenergic release inhibitors	Bethanidine Bretylium Debrisoquine Guanadrel Guanazodine Guancydine Guanethidine Guanoclor Guanoxan
Imidazoline receptor agonists	Moxonidine Rilmenidine Tolonidine
Ganglion-blocking/nicotinic antagonists	Hexamethonium^‡ Mecamylamine Pentolinium Trimethaphan

Peripheral

Indirect

Monoamine oxidase inhibitors	Pargyline^‡
VMAT inhibitors	Bietaserpine Deserpidine Methoserpidine Reserpine Syrosingopine
Tyrosine hydroxylase inhibitors	Metirosine

Direct

α₁-Adrenergic receptor blockers	Doxazosin Ketanserin Indoramin Prazosin Trimazosin Urapidil
Non-selective α-adrenergic receptor blockers	Phentolamine

Otherantagonists

Serotonin receptor antagonists	Ketanserin Lidanserin
Endothelin receptor antagonists (for PHTooltip Pulmonary hypertension)	dual (Aprocitentan,Bosentan,Macitentan (+tadalafil),Riociguat) selective (Ambrisentan (+tadalafil),Sitaxentan,Sotatercept)

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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References