Page last updated: 2024-12-08

dipfluzine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

dipfluzine: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	146001
MeSH ID	M0180717

Synonyms (7)

Synonym
dipfluzine
1-butanone, 4-(4-(diphenylmethyl)-1-piperazinyl)-1-(4-fluorophenyl)-
4-(4-(diphenylmethyl)-1-piperazinyl)-1-(4-fluorophenyl)-1-butanone
4-(4-benzhydrylpiperazin-1-yl)-1-(4-fluorophenyl)butan-1-one
89223-80-3
DTXSID90237580
1-diphenylmethyl-4-[3-(4-fluorobenzoyl)propyl] piperazine

Research Excerpts

Overview

Dipfluzine (Dip) is a promising candidate for the treatment of cerebral vascular diseases. It has 5 metabolites in rat urine and liver microsomes, but their biological activity is still unknown.

Excerpt	Reference	Relevance
"Dipfluzine (Dip) is a promising candidate for the treatment of cerebral vascular diseases and has 5 metabolites (M1∼M5) in rat urine and liver microsomes, but their biological activity is still unknown."	( Vasodilation activity of dipfluzine metabolites in isolated rat basilar arteries and their underlying mechanisms. Guo, W; He, C; Li, S; Wang, H; Wang, T; Wang, X; Wang, Y, 2020)	1.58
"Dipfluzine (Dip) is a novel diphenylpiperazine calcium channel blocker first synthesized in China. "	( Effect of dipfluzine on platelet aggregation and thrombus formation. He, RR; Wang, YL, 1994)	2.13
"Dipfluzine (Dip) is a novel calcium antagonist first developed by Department of Chemistry, Beijing University. "	( Selective vasodilatory effect of dipfluzine on vertebral artery in anesthetized dogs. He, RR; Wang, YL, 1993)	2.01
"Dipfluzine (Dip) is a new derivative of cinnarizine (Cin) first developed by Department of Chemistry, Beijing University. "	( Acute toxicity of dipfluzine and its effects on isolated vascular smooth muscle. Fu, SX; Jin, S; Li, YS; Wang, YL, 1990)	2.06

Toxicity

Excerpt	Reference	Relevance
" The acute iv LD50 of Dip and Cin in mice were 37 and 36 mg/kg, respectively."	( Acute toxicity of dipfluzine and its effects on isolated vascular smooth muscle. Fu, SX; Jin, S; Li, YS; Wang, YL, 1990)	0.61

Pharmacokinetics

Excerpt	Reference	Relevance
" The technique was successfully applied to a pharmacokinetic study of Dip and its metabolites after a single oral administration of Dip (20 mg/kg) to rats."	( Pharmacokinetic evaluation of dipfluzine and its three metabolites in rat plasma using liquid chromatography-mass spectrometry. Guo, W; Li, J; Shi, X; Wang, W; Xiong, C, 2014)	0.69

Bioavailability

Excerpt	Reference	Relevance
" To investigate the feasibility of the co-crystal for improving solubility and a faster dissolution rate in vitro and evaluate the bioavailability and tissue distribution of co-crystal in vivo."	( Preparation, characterization, and evaluation of dipfluzine-benzoic acid co-crystals with improved physicochemical properties. Lin, Y; Wang, J; Yang, C; Yang, H, 2014)	0.66
" The co-crystal solubility, the rate of drug dissolution and the relative bioavailability were approximately 500 times, five times and double that of dipfluzine, respectively."	( Preparation, characterization, and evaluation of dipfluzine-benzoic acid co-crystals with improved physicochemical properties. Lin, Y; Wang, J; Yang, C; Yang, H, 2014)	0.86
" Furthermore, the increased relative bioavailability of co-crystal indicated the potential use in further clinical study."	( Preparation, characterization, and evaluation of dipfluzine-benzoic acid co-crystals with improved physicochemical properties. Lin, Y; Wang, J; Yang, C; Yang, H, 2014)	0.66

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	6 (26.09)	18.2507
2000's	9 (39.13)	29.6817
2010's	6 (26.09)	24.3611
2020's	2 (8.70)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

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	23 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
benzoic acid Benzoic Acid: A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.. benzoic acid : A compound comprising a benzene ring core carrying a carboxylic acid substituent.. aromatic carboxylic acid : Any carboxylic acid in which the carboxy group is directly bonded to an aromatic ring.	2.48	2	benzoic acids	algal metabolite; antimicrobial food preservative; drug allergen; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor; human xenobiotic metabolite; plant metabolite
benzophenone benzophenone : The simplest member of the class of benzophenones, being formaldehyde in which both hydrogens are replaced by phenyl groups.	2.02	1	benzophenones	photosensitizing agent; plant metabolite
isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.	2.03	1	catechols; secondary alcohol; secondary amino compound	beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent
n-vinyl-2-pyrrolidinone N-vinyl-2-pyrrolidinone: monomer of POVIDONE; structure given in first source	2.07	1	pyrrolidin-2-ones
4-hydroxybenzophenone 4-hydroxybenzophenone: RN given refers to parent cpd	2.02	1	benzophenones
ouabain Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.	7.01	1	11alpha-hydroxy steroid; 14beta-hydroxy steroid; 5beta-hydroxy steroid; alpha-L-rhamnoside; cardenolide glycoside; steroid hormone	anti-arrhythmia drug; cardiotonic drug; EC 2.3.3.1 [citrate (Si)-synthase] inhibitor; EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; ion transport inhibitor; plant metabolite
flunarizine Flunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.	6.99	1	diarylmethane
cinnarizine Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.	9.51	23	diarylmethane; N-alkylpiperazine; olefinic compound	anti-allergic agent; antiemetic; calcium channel blocker; geroprotector; H1-receptor antagonist; histamine antagonist; muscarinic antagonist
mocetinostat mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).	2.02	1	aminopyrimidine; benzamides; pyridines; secondary amino compound; secondary carboxamide; substituted aniline	antineoplastic agent; apoptosis inducer; autophagy inducer; cardioprotective agent; EC 3.5.1.98 (histone deacetylase) inhibitor; hepatotoxic agent

Condition	Relationship Strength	Studies
Anterior Circulation Transient Ischemic Attack [description not available]	2.04	1
Ischemic Attack, Transient Brief reversible episodes of focal, nonconvulsive ischemic dysfunction of the brain having a duration of less than 24 hours, and usually less than one hour, caused by transient thrombotic or embolic blood vessel occlusion or stenosis. Events may be classified by arterial distribution, temporal pattern, or etiology (e.g., embolic vs. thrombotic). (From Adams et al., Principles of Neurology, 6th ed, pp814-6)	2.04	1
Brain Swelling [description not available]	2.4	2
Cerebral Ischemia [description not available]	3.1	5
Acute Disease Disease having a short and relatively severe course.	2.01	1
Brain Edema Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)	2.4	2
Brain Ischemia Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.	3.1	5
Injury, Ischemia-Reperfusion [description not available]	2.43	2
Reperfusion Injury Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.	2.43	2
Cerebral Infarction, Middle Cerebral Artery [description not available]	2.02	1
Infarction, Middle Cerebral Artery NECROSIS occurring in the MIDDLE CEREBRAL ARTERY distribution system which brings blood to the entire lateral aspects of each CEREBRAL HEMISPHERE. Clinical signs include impaired cognition; APHASIA; AGRAPHIA; weak and numbness in the face and arms, contralaterally or bilaterally depending on the infarction.	2.02	1
Carotid Artery Thrombosis Blood clot formation in any part of the CAROTID ARTERIES. This may produce CAROTID STENOSIS or occlusion of the vessel, leading to TRANSIENT ISCHEMIC ATTACK; CEREBRAL INFARCTION; or AMAUROSIS FUGAX.	1.98	1
Blood Clot [description not available]	1.98	1
Thrombosis Formation and development of a thrombus or blood clot in the blood vessel.	1.98	1
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	2.38	2

chemdatabank.com