Explore a selection of our essential drug information below, or:
Identification
- Generic Name
- FK352B
- DrugBank Accession Number
- DB06484
- Background
FK352B is a adenosine A1 antagonist that is developed for the treatment of dialysis-induced hypotension.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for FK352B (DB06484)
- Weight
- Average: 389.455
Monoisotopic: 389.173941613 - Chemical Formula
- C23H23N3O3
- Synonyms
- 2-((2R)-1-((2E)-3-(2-PHENYLPYRAZOLO(1,5-A)PYRIDIN-3-YL)PROP-2-ENOYL)PIPERIDIN-2-YL)ACETIC ACID
- 2-PIPERIDINEACETIC ACID, 1-((2E)-1-OXO-3-(2-PHENYLPYRAZOLO(1,5-A)PYRIDIN-3-YL)-2-PROPEN-1-YL)-, (2R)-
- External IDs
- FK-352
- FK352
Pharmacology
- Indication
Investigated for use/treatment in hypertension.
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Not Available
- Mechanism of action
Intradialytic hypotension is a most frequent complication of hemodialysis and may contribute to cardiovascular events and high mortality. There is a hypothesis that an increase in adenosine generation during hemodialysis may cause vasodilation and a decrease in cardiac output, which results in systemic hypotension. The A1 receptors, which are reported to be distributed in the ends of sympathetic nerves, suppress the release of catecholamines from the ends of the nerves. Adenosine selectively inhibits contractions of the rabbit portal vein evoked by adrenergic nerve stimulation via activation of an A1 receptor. This means that adenosine could inhibit constriction of peripheral vessels via the A1 receptors in the ends of the nerves. FK352, a highly selective A1 adenosine receptor antagonist, significantly attenuated LPS-induced reductions in renal blood flow and mean arterial pressure. It may restore the adenosine-induced decline in constriction.
Target Actions Organism AAdenosine receptor A1 antagonistHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Not Available
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- H7CU6R2QEX
- CAS number
- 143881-08-7
- InChI Key
- UWTYIJJJSYDUQM-QFQMRYFISA-N
- InChI
- InChI=1S/C23H23N3O3/c27-21(25-14-6-4-10-18(25)16-22(28)29)13-12-19-20-11-5-7-15-26(20)24-23(19)17-8-2-1-3-9-17/h1-3,5,7-9,11-13,15,18H,4,6,10,14,16H2,(H,28,29)/b13-12+/t18-/m1/s1
- IUPAC Name
- SMILES
- OC(=O)C[C@H]1CCCCN1C(=O)\C=C\C1=C2C=CC=CN2N=C1C1=CC=CC=C1
References
- General References
- Not Available
- External Links
- ChemSpider
- 4946329
Clinical Trials
- Clinical Trials
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Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
- Specific Function
- G protein-coupled adenosine receptor activity
- Gene Name
- ADORA1
- Uniprot ID
- P30542
- Uniprot Name
- Adenosine receptor A1
- Molecular Weight
- 36511.325 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Drug created at March 19, 2008 16:34 / Updated at August 26, 2024 19:22