Guanadrel sulfate is a centrally acting antihypertensive agent. It is a derivative of guanethidine and shares its mechanism of action. Guanadrel sulfate acts by depleting norepinephrine from peripheral sympathetic nerve endings. This results in a decrease in sympathetic nerve activity and a reduction in blood pressure. It is absorbed from the gastrointestinal tract and reaches peak plasma concentrations within 2-4 hours. It is metabolized by the liver and excreted in the urine. Guanadrel sulfate is indicated for the treatment of mild to moderate hypertension. It is generally well-tolerated, but common side effects include dizziness, orthostatic hypotension, and fatigue. Guanadrel sulfate is no longer widely used as a treatment for hypertension due to the availability of safer and more effective alternatives. Research on Guanadrel sulfate is still ongoing, focusing on its potential use in other medical fields, such as pain management and cancer treatment. Guanadrel sulfate's potential for treating pain is explored due to its ability to block nerve transmission. Its potential in cancer treatment arises from its ability to inhibit the growth of cancer cells. However, further research is needed to confirm these potential applications.'
guanadrel sulfate : An organic sulfate salt resulting from the reaction of 2 eq. guanadrel with 1 eq. sulfuric acid. A postganglionic adrenergic blocking agent formerly used for the management of hypertension, it has been largely superseded by other drugs less likely to cause orthostatic hypotension (dizzy spells on standing up or stretching). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 68552 |
| CHEMBL ID | 3184143 |
| CHEBI ID | 5556 |
| SCHEMBL ID | 1649864 |
| MeSH ID | M0308811 |
| Synonym |
|---|
| CHEBI:5556 , |
| 1-(1,4-dioxaspiro[4.5]dec-2-ylmethyl)guanidine sulfate |
| bis{amino[(1,4-dioxaspiro[4.5]dec-2-ylmethyl)amino]methaniminium} sulfate |
| anarel |
| cl-1388r |
| u-28288d |
| hylorel |
| guanadrel sulfate |
| D00607 , |
| guanadrel sulfate (usan) |
| guanidine (1,4-dioxaspiro(4.5)dec-2-ylmethyl)-, sulfate (2:1) |
| (1,4-dioxaspiro(4.5)dec-2-ylmethyl)guanidine sulfate (2:1) |
| hyloride |
| cl 1388r |
| u 28,288d |
| guanadrel sulfate [usan] |
| u 28288d |
| hsdb 6536 |
| HMS1570I16 |
| HMS2097I16 |
| nsc-760062 |
| dtxsid8045432 , |
| dtxcid6025432 |
| tox21_110595 |
| guanadrel sulfate [usan:usp] |
| u-28,288d |
| nsc 760062 |
| unii-mt147rmo91 |
| mt147rmo91 , |
| guanadrel sulfate [vandf] |
| guanadrel sulfate [mart.] |
| guanadrel sulfate [orange book] |
| guanadrel sulfate [usp impurity] |
| guanadrel sulphate |
| guanadrel sulfate [mi] |
| guanidine (1,4-dioxaspiro(4.5)dec-2-ylmethyl)-, sulphate (2:1) |
| 1,4-dioxaspiro(4.5)dec-2-ylmethyl)guanidine sulphate (2:1) |
| guanadrel sulfate [who-dd] |
| 1,4-dioxaspiro(4.5)dec-2-ylmethyl)guanidine sulfate (2:1) |
| guanadrel sulfate [hsdb] |
| CCG-220767 |
| SCHEMBL1649864 |
| guanadrel hemisulfate |
| CHEMBL3184143 |
| sr-01000872677 |
| SR-01000872677-1 |
| HMS3714I16 |
| n-(1,4-dioxaspiro[4.5]dec-2-ylmethyl)guanidine sulfate(2:1) |
| Q27106807 |
| n-(1,4-dioxaspiro[4.5]dec-2-ylmethyl)guanidine hemisulfate |
| guanadrel sulfate (mart.) |
| 1-(1,4-dioxaspiro(4.5)dec-2-ylmethyl)guanidine sulfate |
| guanadrel sulfate (usp impurity) |
| bis(amino((1,4-dioxaspiro(4.5)dec-2-ylmethyl)amino)methaniminium) sulfate |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Role | Description |
|---|---|
| adrenergic antagonist | An agent that binds to but does not activate adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. |
| antihypertensive agent | Any drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| organic sulfate salt | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 12.7448 | 0.0002 | 21.2231 | 8,912.5098 | AID743040 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 3 (60.00) | 24.3611 |
| 2020's | 2 (40.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (18.31) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||