Page last updated: 2024-11-12

ziconotide

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

Description

ziconotide: amino acid sequence in first source; from venom of South Pacific sea cone snail, Conus magus; calcium channel blocker; administered by injection into Cerebrospinal Fluid; Prialt is synthetic form [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

omega-conotoxin MVIIA : A heterodetic cyclic polypeptide consisting of the linear sequence Cys-Lys-Gly-Lys-Gly-Ala-Lys-Cys-Ser-Arg-Leu-Met-Tyr-Asp-Cys-Cys-Thr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-Cys-NH2 with three disulfide bridges between cysteine residues 1-16, 8-20 and 15-25. A neuronal N-type Ca(2+) channel blocker in mammalian and amphibian brain, it blocks release of GABA and glutamate at neuronal synapses. Used as a probe for calcium channel receptors, it is selective for different receptor subtypes. A synthetic form, named ziconotide, is an atypical analgesic agent for the amelioration of severe and chronic pain. [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]

Cross-References

ID SourceID
PubMed CID16135415
CHEMBL ID4594214
CHEBI ID135912
CHEBI ID142406
MeSH IDM0210279

Synonyms (36)

Synonym
gtpl2536
omega-conotoxin m viia (reduced), cyclic (1-16),(8-20),(15-25)-tris(disulfide)
ziconotide
drg-0250
omega-conotoxin mviia, conus magus
omega-conotoxin mviia
l-cysteinyl-l-lysylglycyl-l-lysylglycyl-l-alanyl-l-lysyl-l-cysteinyl-l-seryl-l-arginyl-l-leucyl-l-methionyl-l-tyrosyl-l-alpha-aspartyl-l-cysteinyl-l-cysteinyl-l-threonylglycyl-l-seryl-l-cysteinyl-l-arginyl-l-serylglycyl-l-lysyl-l-cysteinamide cyclic (1-16
omega-conotoxin m viia
snx-111
omega-conopeptide mviia (conus)
CHEBI:135912
cys-lys-gly-lys-gly-ala-lys-cys-ser-arg-leu-met-tyr-asp-cys-cys-thr-gly-ser-cys-arg-ser-gly-lys-cys-nh2
AKOS015994641
unii-7i64c51o16
7i64c51o16 ,
hsdb 7609
ziconotide [usan:inn]
HS-2032
Y-100004
mfcd00145036
omega-conotoxin mviia, >=95% (hplc)
h-cys-lys-gly-lys-gly-ala-lys-cys-ser-arg-leu-met-tyr-asp-cys-cys-thr-gly-ser-cys-arg-ser-gly-lys-cy
150770-63-1
o-conotoxin mviia
.omega.-conotoxin m viia
HY-P0062
CS-0015087
DTXSID60883174 ,
CHEMBL4594214
ziconotida
ziconotidum
n02bg08
chebi:142406
ziconotide (mart.)
dtxcid901323852
AC-8938

Research Excerpts

Toxicity

No drug-related deaths, IT granulomas, or permanent adverse sequelae occurred with ziconotide therapy. Ziconotide is associated with neuropsychiatric AEs, such as cognitive impairment, hallucinations, and changes in mood or consciousness.

ExcerptReferenceRelevance
" Although adverse effects were reported, these appeared to be easily managed through dose reduction or symptomatic treatment."( Adverse effects associated with the intrathecal administration of ziconotide.
Paice, JA; Penn, RD, 2000
)
0.31
" The resulting nonclinical toxicology profile was predictive of human adverse events reported in clinical trials and consistent with ziconotide's pharmacological activity."( Nonclinical safety of ziconotide: an intrathecal analgesic of a new pharmaceutical class.
Beck, JC; de Kater, AW; Shopp, GM; Skov, MJ,
)
0.13
" Safety was assessed via adverse events (AEs), vital signs, and routine laboratory values."( Intrathecal ziconotide for severe chronic pain: safety and tolerability results of an open-label, long-term trial.
Charapata, SG; Dissanayake, S; Ellis, D; Fisher, R; Rauck, R; Wallace, MS, 2008
)
0.35
" No drug-related deaths, IT granulomas, or permanent adverse sequelae occurred with ziconotide therapy."( Intrathecal ziconotide for severe chronic pain: safety and tolerability results of an open-label, long-term trial.
Charapata, SG; Dissanayake, S; Ellis, D; Fisher, R; Rauck, R; Wallace, MS, 2008
)
0.35
" Doses in a range up to maximum no side effect doses were tested for antihyperalgesic effects in rats with hyperalgesia."( CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain.
Cooke, I; Goodchild, CS; Kolosov, A, 2010
)
0.36
"The maximum no side effect dose of leconotide (2 mg/kg intravenously) caused 51."( CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain.
Cooke, I; Goodchild, CS; Kolosov, A, 2010
)
0.36
" It is challenging to use and can induce several and sometimes serious adverse events."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
"To determine whether a low starting dosage of ziconotide, followed by slow titration, decreases the incidence of major adverse events associated with ziconotide when used for intractable cancer pain."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
"Patients with incurable cancer causing chronic pain rated above 6/10 on a numerical scale while receiving high-dose opioid therapy (more than 200 mg/d of oral morphine equivalent) and/or exhibiting severe opioid-related adverse events received intrathecal infusions of ziconotide combined with morphine, ropivacaine, and clonidine."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
" Adverse events were recorded in 57% of them; moderate adverse events occurred in 51%."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
" Determining the relative contributions of each drug to adverse events was difficult, and some of the adverse events manifested as clinical symptoms of a subjective nature."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
"The rates of minor and moderate adverse events were consistent with previous reports."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
"Potentially severe and clinically relevant adverse events (AEs) associated with IT morphine include respiratory depression, tolerance, and granuloma formulation, whereas IT ziconotide is associated with neuropsychiatric AEs, such as cognitive impairment, hallucinations, and changes in mood or consciousness, particularly with high doses and rapid titration."( The Relationship Between the Mechanisms of Action and Safety Profiles of Intrathecal Morphine and Ziconotide: A Review of the Literature.
Webster, LR, 2015
)
0.42
" Ziconotide use is challenging given its adverse effect (AE) profile."( Ziconotide Combination Intrathecal Therapy for Noncancer Pain Is Limited Secondary to Delayed Adverse Effects: A Case Series With a 24-Month Follow-Up.
Hanes, MC; Hayek, SM; Veizi, IE; Wang, C, 2015
)
0.42
"Use of intrathecal admixtures is widespread, but compounding these is sometimes challenging and may result in errors and complications causing super-potency or sub potency adverse events in patients or malfunctions in the pump itself."( Rationale for Prospective Assays of Intrathecal Mixtures Including Morphine, Ropivacaine and Ziconotide: Prevention of Adverse Events and Feasibility in Clinical Practice.
Bazin, C; Boré, F; Devys, C; Dubois, PY; Dupoiron, D; Folliard, C; Kieffer, H; Lebrec, N,
)
0.13
"This study is monocentric and limitations include also its non-randomized nature with no clinical comparison of the rate of adverse events with a refill process without control of each component concentrations."( Rationale for Prospective Assays of Intrathecal Mixtures Including Morphine, Ropivacaine and Ziconotide: Prevention of Adverse Events and Feasibility in Clinical Practice.
Bazin, C; Boré, F; Devys, C; Dubois, PY; Dupoiron, D; Folliard, C; Kieffer, H; Lebrec, N,
)
0.13
" The most common adverse events (≥ 10% of patients overall as of the data cut) were nausea (19."( Effectiveness and Safety of Intrathecal Ziconotide: Interim Analysis of the Patient Registry of Intrathecal Ziconotide Management (PRIZM).
Deer, T; Grigsby, EJ; Huang, IZ; Kim, P; McDowell, GC; Mori, F; Rauck, RL; Saulino, MF; Vanhove, GF; Wallace, M, 2018
)
0.48
" The adverse event profile was consistent with the ziconotide prescribing information."( Effectiveness and Safety of Intrathecal Ziconotide: Interim Analysis of the Patient Registry of Intrathecal Ziconotide Management (PRIZM).
Deer, T; Grigsby, EJ; Huang, IZ; Kim, P; McDowell, GC; Mori, F; Rauck, RL; Saulino, MF; Vanhove, GF; Wallace, M, 2018
)
0.48
" Adverse events were solicited at each visit."( Effectiveness and Safety of Intrathecal Ziconotide: Final Results of the Patient Registry of Intrathecal Ziconotide Management (PRIZM).
Deer, T; Grigsby, EJ; Huang, IZ; Kim, P; McDowell, GC; Rauck, RL; Ryan, R; Saulino, MF; Vanhove, GF; Wallace, M, 2020
)
0.56
" Almost all patients experienced adverse events, the most common of which were nausea (25."( Effectiveness and Safety of Intrathecal Ziconotide: Final Results of the Patient Registry of Intrathecal Ziconotide Management (PRIZM).
Deer, T; Grigsby, EJ; Huang, IZ; Kim, P; McDowell, GC; Rauck, RL; Ryan, R; Saulino, MF; Vanhove, GF; Wallace, M, 2020
)
0.56

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic studies were conducted in rats and cynomologus monkeys to determine the disposition of this compound when it is administered for 24 hr by continuous, constant-rate intravenous infusion."( Pharmacokinetics of SNX-111, a selective N-type calcium channel blocker, in rats and cynomolgus monkeys.
Bowersox, S; Luther, RR; Mandema, J; Miljanich, G; Tarczy-Hornoch, K, 1997
)
0.3
" Pharmacokinetic (PK) parameters were calculated by noncompartmental methods."( Pharmacokinetics and pharmacodynamics of intrathecal ziconotide in chronic pain patients.
Chao, S; Drass, M; Ellis, D; Hale, V; Mayo, M; McGuire, D; O'Connell, D; Wermeling, D, 2003
)
0.32

Bioavailability

ExcerptReferenceRelevance
" Presence of chitosan enhanced the overall bioavailability of ziconotide from intranasal solution and gel formulations."( Delivery of ziconotide to cerebrospinal fluid via intranasal pathway for the treatment of chronic pain.
Jo, SB; Kundu, S; Kushwaha, AS; Manda, P; Murthy, SN; Shivakumar, HN, 2016
)
0.43

Dosage Studied

Future studies are warranted to determine the optimal dosing and titration schedules for ziconotide-baclofen usage. Newer modalities that include patient-controlled analgesia and nocturnal flex dosing have been shown to hold promise of further improvements in ziconocide efficacy and tolerability.

ExcerptRelevanceReference
" SNX-111 reduced the injury-induced calcium accumulation within the ipsilateral cortex in a dose-response fashion when measured at 6, 12, and 48 hours after insult."( Effects of an N-type calcium channel antagonist (SNX 111; Ziconotide) on calcium-45 accumulation following fluid-percussion injury.
Badie, H; Fu, K; Hovda, DA; Luther, RR; Samii, A, 1999
)
0.3
" The combination of ziconotide and morphine produced an additive inhibition of formalin-induced tonic flinch responses and a significant leftward shift of the morphine dose-response curve in the paw pressure test."( Interactions of intrathecally administered ziconotide, a selective blocker of neuronal N-type voltage-sensitive calcium channels, with morphine on nociception in rats.
Bowersox, SS; Gao, D; Pettus, M; Phillips, C; Wang, YX, 2000
)
0.31
" Because mitochondrial dysfunction is easy to assess compared with neurobehavioral endpoints, it might prove useful as an outcome measure to establish therapeutic time windows and dose-response curves in preclinical drug testing."( Improvement in mitochondrial dysfunction as a new surrogate efficiency measure for preclinical trials: dose-response and time-window profiles for administration of the calcium channel blocker Ziconotide in experimental brain injury.
Lee, CP; Muizelaar, JP; Peterson, PL; Verweij, BH; Vinas, FC; Xiong, Y, 2000
)
0.31
"The authors established these time-window profiles and dose-response curves on the basis of mitochondrial outcome measures in a total of 42 rats because there were such low standard deviations in these tests."( Improvement in mitochondrial dysfunction as a new surrogate efficiency measure for preclinical trials: dose-response and time-window profiles for administration of the calcium channel blocker Ziconotide in experimental brain injury.
Lee, CP; Muizelaar, JP; Peterson, PL; Verweij, BH; Vinas, FC; Xiong, Y, 2000
)
0.31
") bolus dosing in rats with adjuvant-induced chronic inflammatory pain of the right hindpaw and to (ii) quantify the inhibitory effects of AM336 relative to MVIIA on K+-evoked SP release from slices of rat spinal cord."( The novel N-type calcium channel blocker, AM336, produces potent dose-dependent antinociception after intrathecal dosing in rats and inhibits substance P release in rat spinal cord slices.
Cabot, PJ; Lewis, RJ; Robertson, AD; Ross, FB; Smith, MT, 2002
)
0.31
"Intrathecal morphine dosing remained constant during the titration phase."( Phase II, open-label, multicenter study of combined intrathecal morphine and ziconotide: addition of ziconotide in patients receiving intrathecal morphine for severe chronic pain.
Fisher, R; Kosek, PS; Leong, M; Schultz, DM; Staats, P; Wallace, MS, 2008
)
0.35
"Multicenter, open-label study with a 4-week morphine titration phase during which ziconotide was held constant and an extension phase during which dosing of either drug could vary."( Open-label, multicenter study of combined intrathecal morphine and ziconotide: addition of morphine in patients receiving ziconotide for severe chronic pain.
Charapata, S; Fakata, KL; Fisher, R; MineHart, M; Webster, LR, 2008
)
0.35
"Ziconotide dosing remained constant during the titration phase; intrathecal morphine titration was based on each patient's daily systemic opioid dose at the study's start."( Open-label, multicenter study of combined intrathecal morphine and ziconotide: addition of morphine in patients receiving ziconotide for severe chronic pain.
Charapata, S; Fakata, KL; Fisher, R; MineHart, M; Webster, LR, 2008
)
0.35
"The purpose of this article was to review the available safety, efficacy and dosing information for ziconotide."( Ziconotide: an update and review.
Day, M; Heavner, JE; Williams, JA, 2008
)
0.35
" It is highly potent, has a steep dose-response curve, a slow onset of action and a narrow margin of safety and responses to dose adjustments are slow."( Ziconotide: an update and review.
Day, M; Heavner, JE; Williams, JA, 2008
)
0.35
" Future studies are warranted to determine the optimal dosing and titration schedules for ziconotide-baclofen usage."( Intrathecal ziconotide and baclofen provide pain relief in seven patients with neuropathic pain and spasticity: case reports.
Burton, AW; Danyo, DA; Frost, S; Glanzer, J; Saulino, M; Solanki, DR, 2009
)
0.35
" The most sensitive parameter was the dosage of ziconotide: using the lower and upper bounds of the average ziconotide dosage observed in the long-term open-label study changed the incremental cost-effectiveness ratio (ICER) to pound 15,500 [pound 8206-25,405] and pound 44,700 [pound 30,541-62, 670]."( Cost-effectiveness of ziconotide in intrathecal pain management for severe chronic pain patients in the UK.
Dewilde, S; Maclaine, GD; Verdian, L, 2009
)
0.35
" One patient with high morphine dosage (20 mg/d), interestingly, did not show any withdrawal symptoms."( Ziconotide: A rapid detoxification protocol for the conversion from intrathecal morphine--the Raffaeli Detoxification Model.
Balestri, M; Caminiti, A; Ferioli, I; Monterubbianesi, MC; Raffaeli, W; Righetti, D; Sarti, D,
)
0.13
" A low initial dosage followed by slow titration may reduce serious adverse events."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
"To determine whether a low starting dosage of ziconotide, followed by slow titration, decreases the incidence of major adverse events associated with ziconotide when used for intractable cancer pain."( Ziconotide adverse events in patients with cancer pain: a multicenter observational study of a slow titration, multidrug protocol.
Bore, F; Brenet, O; Buisset, N; Debourmont, S; Dixmerias, F; Dupoiron, D; Lebrec, N; Lefebvre-Kuntz, D; Monnin, D,
)
0.13
" Larger studies are needed to determine if bolus dosing with ziconotide is a good predictor of response to continuous IT ziconotide via an intrathecal drug delivery system."( Bolus intrathecal injection of ziconotide (Prialt®) to evaluate the option of continuous administration via an implanted intrathecal drug delivery (ITDD) system: a pilot study.
Baranidharan, G; Batterham, AM; Brookes, M; Buchser, E; Crowther, T; Eldabe, S; Gulve, A; Madzinga, G; Mohammed, SI; Perruchoud, C; Radford, H; Simpson, KH,
)
0.13
" However, the maximum recommended dosing and titration schedule provided in the prescribing information may be too aggressive for some patients, and experience has demonstrated that ziconotide is better tolerated with slower titration to a lower maximum dose."( Administering ziconotide and monitoring patients treated with ziconotide: expert opinions.
Hanley, KL; Lokey, KJ; McDowell, GC; Mitchell, AA; Sapienza-Crawford, AJ; Stanton-Hicks, M; Wells, L, 2013
)
0.39
" We introduce a novel dosing strategy to improve patient outcomes and sustainability."( Intrathecal Pharmacology Update: Novel Dosing Strategy for Intrathecal Monotherapy Ziconotide on Efficacy and Sustainability.
Deer, TR; Pope, JE, 2015
)
0.42
" Ziconotide was then initiated with a flex dosing strategy, weighted during nocturnal dosing."( Intrathecal Pharmacology Update: Novel Dosing Strategy for Intrathecal Monotherapy Ziconotide on Efficacy and Sustainability.
Deer, TR; Pope, JE, 2015
)
0.42
"The efficacy and tolerability of monotherapy ziconotide may be improved by using a weighted bolus flex dosing strategy as compared with slow continuous infusions."( Intrathecal Pharmacology Update: Novel Dosing Strategy for Intrathecal Monotherapy Ziconotide on Efficacy and Sustainability.
Deer, TR; Pope, JE, 2015
)
0.42
"We present a novel strategy to deliver ziconotide using a unique continuous infusion flex dosing strategy."( Intrathecal Pharmacology Update: Novel Dosing Strategy for Intrathecal Monotherapy Ziconotide on Efficacy and Sustainability.
Deer, TR; Pope, JE, 2015
)
0.42
" The aim of this review is to provide a comprehensive and clinically relevant summary of the literature on dosing and administration with IT ziconotide in the management of refractory chronic pain, and to describe novel dosing strategies intended to improve clinical outcomes."( Intrathecal Ziconotide: Dosing and Administration Strategies in Patients With Refractory Chronic Pain.
McDowell, GC; Pope, JE, 2016
)
0.43
"Newer modalities that include patient-controlled analgesia and nocturnal flex dosing have been shown to hold promise of further improvements in ziconotide efficacy and tolerability."( Intrathecal Ziconotide: Dosing and Administration Strategies in Patients With Refractory Chronic Pain.
McDowell, GC; Pope, JE, 2016
)
0.43
"Ziconotide use in intrathecal drug therapy (IDT) has been limited by dosing related side effects."( Use of Low Dose Ziconotide as First-Line Intrathecal Monotherapy.
Argoff, C; Peng, S; Pilitsis, JG; Prusik, J, 2017
)
0.46
" Using a conservative dosing strategy, we were able to effectively treat 53% of patients."( Use of Low Dose Ziconotide as First-Line Intrathecal Monotherapy.
Argoff, C; Peng, S; Pilitsis, JG; Prusik, J, 2017
)
0.46
" Of special concern regarding safety is the partial incongruity between dosing statements in the Summary of Product Characteristics and novel low-dosage, slow uptitration recommendations."( Do the potential benefits outweigh the risks? An update on the use of ziconotide in clinical practice.
Bäckryd, E, 2018
)
0.48
" The recovery of spatial memory, besides a reduction of serum leptin levels, allied to central and peripheral elevation of the anti-inflammatory cytokine IL-10, was solely modulated by CTK 01512-2, dosed intrathecally."( Beneficial Effects of the Calcium Channel Blocker CTK 01512-2 in a Mouse Model of Multiple Sclerosis.
Campos, MM; da Costa, JC; Gomez, MV; Greggio, S; Silva, RBM; Venturin, GT, 2018
)
0.48
" For both morphine and ziconotide, the PACC guidelines recommend conservative initial dosing strategies."( Intrathecal Therapy for Chronic Pain: A Review of Morphine and Ziconotide as Firstline Options.
Deer, TR; Hanes, MC; McDowell, GC; Pope, JE, 2019
)
0.51
"In all dosing regimens, ziconotide significantly decreased the seizure frequency and also delayed the latency period compared with control."( Intracerebroventricular administration of N-type calcium channel blocker ziconotide displays anticonvulsant, anxiolytic, and sedative effects in rats: A preclinical and pilot study.
Bozorgi, H; Budde, T; Zamani, M, 2020
)
0.56
" Before a consensus process can formally begin, the group called for additional European prospective studies to investigate ziconotide in low-and-slow dosing strategies, in different patient settings."( Intrathecal pain management with ziconotide: Time for consensus?
De Negri, P; Dupoiron, D; Likar, R; Matis, G; Rasche, D; Zuidema, X, 2021
)
0.62
" The aim of this project is to conduct a budget impact analysis to estimate the costs or savings associated with the changes in ziconotide dosage in addition to its use in combination with morphine for the management of cancer pain."( Ziconotide for the Management of Cancer Pain: A Budget Impact Analysis.
Black, S; Copley, S; Duarte, R; Dupoiron, D; Eldabe, R; Eldabe, S; Kansal, A; Lambe, T, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC50 (µMol)0.55000.04004.113710.0000AID248800; AID248976
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (4)

Processvia Protein(s)Taxonomy
modulation of chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
response to amyloid-betaVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
amyloid-beta bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
protein bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
ATP bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
synapseVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
neuronal cell bodyVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1731258Toxicity in Sprague-Dawley rat assessed as induction of hyperactivity at 1 microg/kg, IT
AID1731256Toxicity in Sprague-Dawley rat assessed as induction of drowsiness at 1 microg/kg, IT
AID1731257Toxicity in Sprague-Dawley rat assessed as induction of abnormal gait at 1 microg/kg, IT
AID248976In vitro antagonism of N-type calcium channels expressed in PC12 cells was determined as the increase in intracellular calcium influx in the presence of 10 uM nifedipine2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.
AID248800In vitro antagonism of N-type calcium channels expressed in PC12 cells was determined as the increase in intracellular calcium influx2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.
AID1731254Toxicity in Sprague-Dawley rat assessed as induction of dizziness at 1 microg/kg, IT
AID1731252Antinociceptive activity in Sprague-Dawley rat model of formalin-induced nociception pain assessed as reduction in pain behaviour by measuring less lifting of formalin injected hind paw during acute phase at 1 microg/kg, IT measured for 9 mins
AID1731275Antinociceptive activity in Sprague-Dawley rat model of formalin-induced nociception pain assessed as reduction in pain behaviour by measuring less lifting of formalin injected hind paw during inflammatory phase at 1 microg/kg, IT
AID1731253Toxicity in Sprague-Dawley rat assessed as induction of ataxia at 1 microg/kg, IT
AID1731255Toxicity in Sprague-Dawley rat assessed as induction of tremor at 1 microg/kg, IT
AID1346693Rat Cav2.2 (Voltage-gated calcium channels)2000The Journal of biological chemistry, Nov-10, Volume: 275, Issue:45
Novel omega-conotoxins from Conus catus discriminate among neuronal calcium channel subtypes.
AID1346724Rat Cav2.1 (Voltage-gated calcium channels)2000The Journal of biological chemistry, Nov-10, Volume: 275, Issue:45
Novel omega-conotoxins from Conus catus discriminate among neuronal calcium channel subtypes.
AID1346693Rat Cav2.2 (Voltage-gated calcium channels)2006Biochemical pharmacology, Sep-14, Volume: 72, Issue:6
Pharmacological characterization of recombinant N-type calcium channel (Cav2.2) mediated calcium mobilization using FLIPR.
AID1346686Human Cav2.2 (Voltage-gated calcium channels)2002The Journal of neuroscience : the official journal of the Society for Neuroscience, Jan-01, Volume: 22, Issue:1
Identification and characterization of novel human Ca(v)2.2 (alpha 1B) calcium channel variants lacking the synaptic protein interaction site.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (277)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's69 (24.91)18.2507
2000's98 (35.38)29.6817
2010's82 (29.60)24.3611
2020's28 (10.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (4.90%)5.53%
Reviews52 (16.99%)6.00%
Case Studies28 (9.15%)4.05%
Observational4 (1.31%)0.25%
Other207 (67.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of a Structured Algorithm for Intrathecal Bolus Doses of Ziconotide (Prialt®)- The Swedish Ziconotide Bolus Study [NCT01373983]Phase 426 participants (Actual)Interventional2011-08-31Completed
Phase II Study of Intrathecal Ziconotide for the Treatment of Neuropathic Pain in Patients With Cancer [NCT00996983]Phase 216 participants (Anticipated)Interventional2009-09-30Active, not recruiting
Patient Registry of Intrathecal Ziconotide Management (PRIZM): An Open-Label, Long Term, Multi-Center, Observational Study of PRIALT® (Ziconotide) Solution, Intrathecal Infusion, in Patients With Severe Chronic Pain [NCT01888120]93 participants (Actual)Observational [Patient Registry]2013-07-31Completed
A Phase 4, Randomized, Double-blind, Placebo-controlled, Cross-over Clinical Trial of a Single Shot of Intrathecal Ziconotide for the Treatment of Chronic, Medically Refractory Pain From Painful Peripheral Neuropathy or Myelopathy [NCT01992562]Phase 40 participants (Actual)Interventional2014-01-31Withdrawn(stopped due to Logistical issues with study process and recruitment)
OP2C : Prialt® Observatory in Clinical Practice [NCT04321408]300 participants (Anticipated)Observational [Patient Registry]2020-07-10Recruiting
A Multicenter Phase II/III, Placebo-Controlled Study of SNX-111 Administered Intrathecally to Cancer and AIDS Patients With Chronic Pain [NCT00002160]Phase 2100 participants InterventionalCompleted
An Open-Label, Long-Term, Multi-Center, Intrathecal Ziconotide (PRIALT) Effectiveness and Safety Trial (ZEST) in Patients With Chronic Severe Pain [NCT00076544]Phase 3300 participants Interventional2004-02-29Completed
A Randomized, Double-Blind, Placebo-Controlled Study of Intrathecal Ziconotide in Adults With Severe Chronic Pain [NCT00047749]Phase 3220 participants Interventional2002-08-31Completed
Prospective Study of Conservative Ziconotide Dosing as a First-Line Intrathecal Drug Therapy for Neuropathic Pain [NCT03321955]Phase 413 participants (Actual)Interventional2016-11-03Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]