Compounds > ulixacaltamide
Page last updated: 2024-11-13

ulixacaltamide

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

Description

Z944: a T-type calcium channel antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44540045
CHEMBL ID3934636
CHEBI ID194339
SCHEMBL ID4271563

Synonyms (31)

Synonym
FT-0664015
n-({1-[2-(tert-butylamino)-2-oxoethyl]piperidin-4-yl}methyl)-3-chloro-5-fluorobenzamide
CHEBI:194339
z944
ulixacaltamida
z-944
z 944
1199236-64-0
ulixacaltamide
ulixacaltamidum
n-((1-(2-(tert-butylamino)-2-oxoethyl)piperidin-4-yl)methyl)-3-chloro-5-fluorobenzamide
prax-944
prax944
gtpl7718
n-[[1-[2-(tert-butylamino)-2-oxoethyl]piperidin-4-yl]methyl]-3-chloro-5-fluorobenzamide
SCHEMBL4271563
DTXSID60659275
AKOS027446732
CHEMBL3934636 ,
bdbm50192689
4-[[(3-chloro-5-fluorobenzoyl)amino)methyl]-n-(1,1-dimethylethyl)-1-piperidineacetamide
Q27089278
4-(((3-chloro-5-fluorobenzoyl)amino)methyl)-n-(1,1-dimethylethyl)-1-piperidineacetamide
QT2PJH89C3 ,
ulixacaltamide [inn]
1-piperidineacetamide, 4-(((3-chloro-5-fluorobenzoyl)amino)methyl)-n-(1,1-dimethylethyl)-
DZR ,
MS-26311
unii-qt2pjh89c3
CS-0078307
HY-120546
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
T-type calcium channel blockerAny agent that interferes with the activity of T-type calcium channels.
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
[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]

Drug Classes (5)

ClassDescription
piperidines
benzamides
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
monofluorobenzenesAny member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent.
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
[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 Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)IC50 (µMol)0.03700.03700.89152.5000AID1316446; AID1325717
Voltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)IC50 (µMol)0.07300.03201.04793.6000AID1316439; AID1325718
Voltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)IC50 (µMol)0.08600.08600.65472.5000AID1316437; AID1325719
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
sinoatrial node developmentVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
response to nickel cationVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
regulation of membrane potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
calcium ion importVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
SA node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
AV node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
SA node cell to atrial cardiac muscle cell signalingVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
AV node cell to bundle of His cell signalingVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
muscle contractionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
muscle organ developmentVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
myoblast fusionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
regulation of heart contractionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
aldosterone biosynthetic processVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cellular response to hormone stimulusVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cortisol biosynthetic processVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cellular response to potassium ionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
regulation of membrane potentialVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
calcium ion importVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
inorganic cation transmembrane transportVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
positive regulation of acrosome reactionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
signal transductionVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
neuronal action potentialVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
sleepVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
low voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
scaffold protein bindingVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated monoatomic ion channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
protein bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
low voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
metal ion bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
scaffold protein bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
protein bindingVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
cytoplasmVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
synapseVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent T-type calcium channel subunit alpha-1GHomo sapiens (human)
plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent T-type calcium channel subunit alpha-1IHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1325719Inhibition of human CaV 3.3 by manual patch clamp assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.
AID1316446Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.
AID1316439Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.
AID1325718Inhibition of human CaV 3.2 by manual patch clamp assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.
AID1325717Inhibition of human CaV 3.1 by manual patch clamp assay2016Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
Structure-Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers.
AID1316437Inhibition of T-type calcium channel Cav3.3 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.
AID1346702Human Cav3.3 (Voltage-gated calcium channels)2012Science translational medicine, Feb-15, Volume: 4, Issue:121
T-type calcium channel blockers that attenuate thalamic burst firing and suppress absence seizures.
AID1346720Human Cav3.2 (Voltage-gated calcium channels)2012Science translational medicine, Feb-15, Volume: 4, Issue:121
T-type calcium channel blockers that attenuate thalamic burst firing and suppress absence seizures.
AID1346719Human Cav3.1 (Voltage-gated calcium channels)2012Science translational medicine, Feb-15, Volume: 4, Issue:121
T-type calcium channel blockers that attenuate thalamic burst firing and suppress absence seizures.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's15 (88.24)24.3611
2020's2 (11.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 41.41

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index41.41 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index59.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (41.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
capsaicin
ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.		2.110capsaicinoidnon-narcotic analgesic;
TRPV1 agonist;
voltage-gated sodium channel blocker
np 118809
1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one: an N-type calcium channel blocker; structure in first source		2.1710
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.1710maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
nnc 55-0396
NNC 55-0396: a calcium channel blocker with high selectivity for CaV3 channels over high voltage activated channels; structure in first source. NNC 55-0396 dihydrochloride : The dihydrochloride salt of NNC 55-0396. It is a stable analogue of mibefradil and a highly selective T-type calcium channel blocker.		2.1710hydrochlorideangiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
potassium channel blocker;
T-type calcium channel blocker
piperidines
Piperidines: A family of hexahydropyridines.		4.23150
ConditionIndicatedRelationship StrengthStudiesTrials
Absence Seizure Disorder
[description not available]		03.3960
Epilepsy, Absence
A seizure disorder usually occurring in childhood characterized by rhythmic electrical brain discharges of generalized onset. Clinical features include a sudden cessation of ongoing activity usually without loss of postural tone. Rhythmic blinking of the eyelids or lip smacking frequently accompanies the SEIZURES. The usual duration is 5-10 seconds, and multiple episodes may occur daily. Juvenile absence epilepsy is characterized by the juvenile onset of absence seizures and an increased incidence of myoclonus and tonic-clonic seizures. (Menkes, Textbook of Child Neurology, 5th ed, p736)		03.3960
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.6580
Aura
[description not available]		02.1310
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.1310
Absence Seizure
[description not available]		02.8330
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.		02.8330
Ache
[description not available]		02.5720
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		02.5720
Age-Related Memory Disorders
[description not available]		02.5520
Dementia Praecox
[description not available]		02.1710
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		02.5520
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		02.1710
Convulsive Generalized Seizure Disorder
[description not available]		02.2110
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.2110
Nerve Pain
[description not available]		02.1310
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.1310