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Identification
- Generic Name
- BF-1
- DrugBank Accession Number
- DB06029
- Background
BF-1 is an investigational 5-HT2B receptor antagonist developed for the prophylaxis of Migraines.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
Structure for BF-1 (DB06029)
- Weight
- Average: 367.51
Monoisotopic: 367.160600223 - Chemical Formula
- C22H25NO2S
- Synonyms
- PIPERIDINE, 4-(6-ETHOXY-1-METHOXY-9H-THIOXANTHEN-9-YLIDENE)-1-METHYL-
Pharmacology
- Indication
Investigated for use/treatment in migraine and cluster headaches.
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Not Available
- Mechanism of action
BF-1 is highly selective and potent 5-HT2B receptor which is being developed for the reduction of the frequency and intensity of migraine attacks. BF-1 intervenes at an early stage of the chemical cascade causing the migraine attacks. The compound prevents the release of second messengers, which initiate a self reinforcing inflammatory cascade ultimately perceived by the patient as migraine headache. Drugs available on the market for the prevention of migraine attacks generally cause severe side effects, causing most patients to discontinue the treatment before a positive therapeutic outcome is obtained. In contrast to the latter group of drugs, BF-1 exhibits a very high receptor selectivity, due to which, according to the scientists at Biofrontera, the risk of side effects can be considered very small.
Target Actions Organism U5-hydroxytryptamine receptor 2B Not Available Humans - 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
- 366ZW99DGL
- CAS number
- 518980-66-0
- InChI Key
- ANZVBVKYXOGOQC-UHFFFAOYSA-N
- InChI
- InChI=1S/C22H25NO2S/c1-4-25-16-8-9-17-20(14-16)26-19-7-5-6-18(24-3)22(19)21(17)15-10-12-23(2)13-11-15/h5-9,14H,4,10-13H2,1-3H3
- IUPAC Name
- SMILES
- CCOC1=CC2=C(C=C1)C(=C1CCN(C)CC1)C1=C(OC)C=CC=C1S2
References
- General References
- Schmitz B, Ullmer C, Segelcke D, Gwarek M, Zhu XR, Lubbert H: BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol. 2015 Mar 15;751:73-80. doi: 10.1016/j.ejphar.2015.01.043. Epub 2015 Feb 7. [Article]
- External Links
- ChemSpider
- 8462506
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
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin) (PubMed:18703043, PubMed:23519210, PubMed:7926008, PubMed:8078486, PubMed:8143856, PubMed:8882600). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances (PubMed:12970106, PubMed:18703043, PubMed:23519210, PubMed:23519215, PubMed:24357322, PubMed:28129538, PubMed:7926008, PubMed:8078486, PubMed:8143856). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors (PubMed:23519215, PubMed:28129538, PubMed:8078486, PubMed:8143856, PubMed:8882600). Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways (PubMed:23519215, PubMed:28129538). Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores (PubMed:18703043, PubMed:23519215, PubMed:28129538, PubMed:8078486, PubMed:8143856, PubMed:8882600). Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain (By similarity). Plays a role in the regulation of behavior, including impulsive behavior (PubMed:21179162). Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine (By similarity)
- Specific Function
- G protein-coupled serotonin receptor activity
- Gene Name
- HTR2B
- Uniprot ID
- P41595
- Uniprot Name
- 5-hydroxytryptamine receptor 2B
- Molecular Weight
- 54297.41 Da
Drug created at November 18, 2007 18:29 / Updated at July 24, 2024 23:35