Compounds > pazinaclone
Page last updated: 2024-12-06

pazinaclone

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

Description

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

Cross-References

ID SourceID
PubMed CID59743
SCHEMBL ID120974
MeSH IDM0167815

Synonyms (39)

Synonym
dn-2327
pazinaclone
a-77000
1,4-dioxa-8-azaspiro(4.5)decane, 8-((2-(7-chloro-1,8-naphthyridin-2-yl)-2,3-dihydro-3-oxo-1h-isoindol-1-yl)acetyl)-
(+-)-8-((2-(7-chloro-1,8-naphthyridin-2-yl)-3-oxo-1-isoindolinyl)acetyl)-1,4-dioxa-8-azaspiro(4.5)decane
(+-)-2-(7-chloro-1,8-naphthyridin-2-yl)-3-(((1,4-dioxa-8-azaspiro(4.5)dec-8-yl)carbonyl)methyl)-1-isoindolinone
a 77000
dn 2327
pazinaclone [usan:inn]
1,4-dioxa-8-azaspiro(4.5)decane, 8-((2-(7-chloro-1,8-naphthyridin-2-yl)-2,3-dihydro-3-oxo-1h-isoindol-1-yl)acetyl)-, (+-)-
OPREA1_524484
pazinaclone (usan/inn)
D05378
103255-66-9
2-(7-chloro-1,8-naphthyridin-2-yl)-3-[2-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-2-oxoethyl]-3h-isoindol-1-one
2-(7-chloro-1,8-naphthyridin-2-yl)-3-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-2-oxoethyl]isoindolin-1-one
unii-m9t85b75l9
unii-2rl7k6wx26
(r)-pazinaclone
mhk03047ij ,
unii-mhk03047ij
FT-0631024
AKOS015913910
1,4-dioxa-8-azaspiro(4.5)decane, 8-((2-(7-chloro-1,8-naphthyridin-2-yl)-2,3-dihydro-3-oxo-1h-isoindol-1-yl)acetyl)-, (+/-)-
pazinaclone [inn]
pazinaclone [who-dd]
(+/-)-8-((2-(7-chloro-1,8-naphthyridin-2-yl)-3-oxo-1-isoindolinyl)acetyl)-1,4-dioxa-8-azaspiro(4.5)decane
pazinaclone [mi]
pazinaclone [usan]
1h-isoindol-1-one, 2-(7-chloro-1,8-naphthyridin-2-yl)-3-(2-(1,4-dioxa-8-azaspiro(4.5)dec-8-yl)-2-oxoethyl)-2,3-dihydro-
(+/-)-2-(7-chloro-1,8-naphthyridin-2-yl)-3-(((1,4-dioxa-8-azaspiro(4.5)dec-8-yl)carbonyl)methyl)-1-isoindolinone
SCHEMBL120974
DPGKFACWOCLTCA-UHFFFAOYSA-N
2-(7-chloro-1,8-naphthyridin-2-yl)-3-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)carbonylmethylisoindolin-1-one
1h-isoindol-1-one, 2-(7-chloro-1,8-naphthyridin-2-yl)-3-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-2-oxoethyl]-2,3-dihydro-;1h-isoindol-1-one, 2-(7-chloro-1,8-naphthyridin-2-yl)-3-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-2-oxoethyl]-2,3-dihydro-
2-(7-chloro-1,8-naphthyridin-2-yl)-3-(2-oxo-2-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)ethyl)isoindolin-1-one
Q7157014
A921483
DTXSID70869388

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Simultaneous model-dependent analysis of the intravenous plasma profiles for parent drug and metabolite suggested stereoselectivity of the active metabolite MII with shorter formation half-life for (S)-MII."( Differences in the stereoselective pharmacokinetics of pazinaclone (DN-2327), a new anxiolytic, and its active metabolite after intravenous and oral single doses to dogs.
Bopp, BA; Granneman, GR; Hussein, Z; Mulford, DJ, )		0.38

Bioavailability

ExcerptReferenceRelevance
" About 60, 75 and 48% of the radioactivity dosed was absorbed in rats, dogs and monkeys, respectively, whereas the bioavailability in rats, dogs and monkeys was less than 1, 34 and 10%, respectively, indicating that DN-2327 had been subjected to the first pass effect."( Disposition of DN-2327, a new anxiolytic, in rats, dogs, and monkeys.
Kondo, T; Kurata, Y; Yoshida, K; Yoshimura, Y, 1995)		0.29

Dosage Studied

In rats, the AUCs for the parent compound after a 3000 mg/kg oral dose of S-pazinaclone were about 9-fold. Of the two polymorphs, forms 1 and 2 with particle size of < or = 5 microns, the oral absorption of form 2 in rats was more efficient than that of form 1 at 1000mg/kg.

ExcerptRelevanceReference
"The disposition of DN-2327 after oral dosing of 14C-labeled DN-2327 ([14C]DN-2327) to rats, dogs and monkeys was studied."( Disposition of DN-2327, a new anxiolytic, in rats, dogs, and monkeys.
Kondo, T; Kurata, Y; Yoshida, K; Yoshimura, Y, 1995)		0.29
" In rats, the AUCs for the parent compound after a 3000 mg/kg oral dose of S-pazinaclone were about 9-fold (males) and 4-fold (females) greater than those after dosing of R-pazinaclone at 500 mg/kg."( Enantiomeric toxicokinetics of the new isoindoline anxiolytic pazinaclone in rats and dogs.
Kondo, T; Tanayama, S; Yamamoto, M; Yoshida, K, 1996)		0.76
" Of the two polymorphs, forms 1 and 2 with particle size of < or = 5 microns, the oral absorption of form 2 in rats was more efficient than that of form 1 at 1000 mg/kg: AUCs of pazinaclone after dosing of form 1 and 2 were 489 and 965 ng."( Absorption of the anxiolytic pazinaclone in animals as a criterion for species selection for toxicity studies.
Kondo, T; Tanayama, S; Yoshida, K, 1996)		0.78
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (4.76)18.7374
1990's19 (90.48)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's1 (4.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.97

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.

MetricThis Compound (vs All)
Research Demand Index21.97 (24.57)
Research Supply Index3.22 (2.92)
Research Growth Index5.89 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (9.09%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.3920amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.3711organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
baclofen
[no description available]		1.9910amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
barbital
5,5-diethylbarbituric acid : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by two ethyl groups. Formerly used as a hypnotic (sleeping aid).		1.9910barbituratesdrug allergen
buspirone
Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.		2.8940azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		3.36701,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		2.8940ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
pentobarbital
Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.		2.3820barbituratesGABAA receptor agonist
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		2.3820organic heterobicyclic compound;
organonitrogen heterocyclic compound
yohimbine
Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.		1.9710methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
phthalimidine
phthalimidine: structure given in first source. isoindolin-1-one : A member of the class of isoindoles that is 2,3-dihydro-1H-isoindole in which the hydrogens at positon 1 are replaced by an oxo group.		2.4110gamma-lactam;
isoindoles
ConditionIndicatedRelationship StrengthStudiesTrials
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		01.9810
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		01.9910
Chemical Dependence
[description not available]		01.9910
Drug Withdrawal Symptoms
[description not available]		01.9910
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		01.9910
Substance-Related Disorders
Disorders related to substance use or abuse.		01.9910
Blood Pressure, High
[description not available]		01.9910
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		01.9910
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		01.9910
Absence Seizure
[description not available]		01.9710
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		01.9710
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		01.9710
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		01.9710
Aggression
Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.		01.9710