Arcaine
(Synonyms: ARC)
Arcaine (ARC) is a competitive NMDA receptor polyamine site antagonist and Agmatinase inhibitor. Arcaine inhibits NOS. Arcaine shows anticonvulsant activity and induces state-dependent inhibitory avoidance memory impairment involving the opioid system. Arcaine can be used in research on alcohol use disorder.
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- No. CAS: 544-05-8
- Fòrmula: C6H16N6
- Peso molecular:172.24
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Descripciòn
Arcaine (ARC) is a competitive NMDA receptor polyamine site antagonist and Agmatinase inhibitor. Arcaine inhibits NOS. Arcaine shows anticonvulsant activity and induces state-dependent inhibitory avoidance memory impairment involving the opioid system. Arcaine can be used in research on alcohol use disorder[1][2][3][4][5][6][7][8].
IC50 & Target
[4]|
NMDA Receptor |
In Vitro
Glutamate Release or ReceptorsOthers
Glutamate Release or Receptors
Arcaine (10-300 μM) blocks NMDA receptor channels in a voltage-dependent manner in cultured rat hippocampal neuron outside-out patches, with an IC50 of 81 μM at -60 mV and a Woodhull KD(0) of 0.78 mM; relief of block at large negative potentials is consistent with a permeant channel blocker[1].
Arcaine blocks NMDA-evoked currents in cultured rat hippocampal neurons with a KD of 61 µM at -60 mV through a strongly voltage-dependent open-channel mechanism[7].
Arcaine blocks NMDA-evoked currents in cultured rat hippocampal neurons with a KD of 61 µM at -60 mV through a strongly voltage-dependent open-channel mechanism[7].
Others
Arcaine reduces apparent single-channel amplitude in a concentration- and voltage-dependent manner, with estimated open-channel binding and unbinding rates of 4.4 × 108 M-1 s-1 and 1.8 × 104 s-1[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Glutamate Release or ReceptorsOthers
Glutamate Release or Receptors
Arcaine (32-100 µg; i.c.v.; once daily 10 min before the kindling stimulus; until five cumulative stage 5 seizures) at 100 µg, but not 32 µg, delays amygdala-kindling development by increasing trials to first and fifth stage 5 seizures without altering afterdischarge duration[2].
Others
Arcaine (10-100 μg; i.c.v.; single administration) alone produces dose-dependent CNS behavioural effects in healthy female Laca mice, ranging from no effect at 10-25 μg to hyperactivity, convulsions, and delayed paralysis at higher doses[3].
Arcaine (10-50 μg; i.c.v.; single co-administration with spermine 100 μg) potentiates early clonic convulsions at all tested doses while potentiating late-phase excitation at 10 μg and reducing it at 25-50 μg in female Laca mice with spermine-induced neurotoxicity/CNS excitation and convulsions[3].
Arcaine (10-30 mg/kg; i.p.; single injection immediately after training) impairs recall of step-down inhibitory avoidance in adult male Wistar rats without altering open-field crossing or rearing[4].
Arcaine (30 mg/kg; i.p.; immediately after training and/or 30 min before testing) produces state-dependent recall because pretesting Arcaine reverses the recall impairment caused by post-training Arcaine in adult male Wistar rats in the step-down inhibitory avoidance task[4].
Arcaine (30 mg/kg; i.p.; 0, 3, 6, or 9 h post-training; 30 min before testing) induces state-dependent memory retrieval in male adult Wistar rats with a one-trial step-down inhibitory avoidance memory task[5].
Arcaine (10 mg/kg; i.p.; single injection; immediately after training) impairs contextual and auditory fear conditioning in male Wistar rats with a fear conditioning memory model without altering novel-context freezing[6].
Arcaine (25 μg/mouse; i.c.v.; single administration) alone produces an anti-nociceptive response in the mouse tail-flick assay at 20 minutes after i.c.v. administration[8].
Arcaine (25 μg/mouse; i.c.v.; single administration; 10 minutes before ethanol 1 g/kg i.p.) potentiates ethanol-induced anti-nociception in mice, increasing tail-flick latency at 20 and 40 minutes[8].
Arcaine (10-50 μg; i.c.v.; single co-administration with spermine 100 μg) potentiates early clonic convulsions at all tested doses while potentiating late-phase excitation at 10 μg and reducing it at 25-50 μg in female Laca mice with spermine-induced neurotoxicity/CNS excitation and convulsions[3].
Arcaine (10-30 mg/kg; i.p.; single injection immediately after training) impairs recall of step-down inhibitory avoidance in adult male Wistar rats without altering open-field crossing or rearing[4].
Arcaine (30 mg/kg; i.p.; immediately after training and/or 30 min before testing) produces state-dependent recall because pretesting Arcaine reverses the recall impairment caused by post-training Arcaine in adult male Wistar rats in the step-down inhibitory avoidance task[4].
Arcaine (30 mg/kg; i.p.; 0, 3, 6, or 9 h post-training; 30 min before testing) induces state-dependent memory retrieval in male adult Wistar rats with a one-trial step-down inhibitory avoidance memory task[5].
Arcaine (10 mg/kg; i.p.; single injection; immediately after training) impairs contextual and auditory fear conditioning in male Wistar rats with a fear conditioning memory model without altering novel-context freezing[6].
Arcaine (25 μg/mouse; i.c.v.; single administration) alone produces an anti-nociceptive response in the mouse tail-flick assay at 20 minutes after i.c.v. administration[8].
Arcaine (25 μg/mouse; i.c.v.; single administration; 10 minutes before ethanol 1 g/kg i.p.) potentiates ethanol-induced anti-nociception in mice, increasing tail-flick latency at 20 and 40 minutes[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 300-400 g)[2]
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Dosage:32 µg and 100 µg
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Administration:i.c.v. over 60 s in 10 µL sterile water; once daily 10 min before the kindling stimulus; until five cumulative stage 5 seizures
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Result:Increased the number of trials required to reach the first stage 5 and fifth stage 5 seizure milestones compared with vehicle and the 32 µg dose; 32 µg had no significant effect.
The increased trials occurred across the stage 3-to-5 interstage interval.
Did not affect afterdischarge duration at either dose.
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Animal Model:Laca (female, 20-25 g)[3]
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Dosage:10, 25, 50, or 100 μg
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Administration:i.c.v.; single administration
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Result:At 10 and 25 μg, no behavioural changes occurred up to four days after injection.
At 50 μg, slight hyperactivity occurred for several hours; within 24 h, approximately half of the mice developed abnormal gait with high carriage lasting two to three days.
At 100 μg, hyperactivity, ataxia, hyperexcitability, and vocalization occurred for several hours; within two to four hours, approximately half of the mice developed face-washing and head-scratching and experienced non-fatal clonic and extensor tonic convulsions.
These convulsions eased approximately 6 h after injection, but within 24 h mice developed tip-toe walking that progressed within two to three days to front or hind limb paralysis and a moribund state.
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Animal Model:Laca (female, 20-25 g)[3]
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Dosage:10, 25, or 50 μg
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Administration:i.c.v.; single co-administration with spermine 100 μg
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Result:Mean clonic episodes per animal were 2.43 for 10 μg (n = 23), 4.76 for 25 μg (n = 34), and 3.32 for 50 μg (n = 19).
At 10 μg, second-phase body tremor and tonic convulsions were potentiated, whereas at 25 and 50 μg the development of these second-phase effects was reduced; the 25 μg effect is shown in Figure 1.
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Animal Model:Wistar (adult male, 200-250 g)[4]
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Dosage:1 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.p.; single injection immediately after training
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Result:Post-training dosing at 10 and 30 mg/kg decreased step-down latencies compared with control; 1 mg/kg did not.
Open-field exploratory activity was 1 mg/kg crossing 24.21, rearing 6.71, N = 14; 10 mg/kg crossing 22.28, rearing 9.00, N = 14; 30 mg/kg crossing 28.64, rearing 9.50, N = 14.
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Animal Model:Wistar (adult male, 200-250 g)[4]
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Dosage:30 mg/kg (immediately after training and/or 30 min before testing)
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Administration:i.p.; immediately after training and/or 30 min before testing
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Result:Step-down latency decreased after post-training administration alone.
Performance was not impaired by pretesting administration alone.
The deficit induced by post-training administration was reversed by pretesting administration.
Open-field exploratory activity: PBS/pretesting crossing 19.00, rearing 7.00, N = 12; post-training/PBS crossing 20.91, rearing 8.16, N = 12; post-training/pretesting crossing 18.66, rearing 5.16, N = 12.
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Animal Model:Wistar (adult male, 200-250 g)[4]
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Dosage:30 mg/kg (Arcaine; immediately after training and/or 30 min before testing); 0.03 mg/kg (MK-801; immediately after training and/or 30 min before testing)
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Administration:i.p.; immediately after training and/or 30 min before testing
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Result:Step-down latency decreased after post-training administration.
The deficit induced by post-training administration was reversed by pretesting administration.
Pretesting MK-801 also reversed the deficit induced by post-training administration, and pretesting administration reversed the deficit induced by post-training MK-801.
Open-field exploratory activity: post-training/PBS crossing 24.26, rearing 12.06, N = 15; post-training/pretesting crossing 23.52, rearing 10.94, N = 17; post-training/MK-801 crossing 27.64, rearing 16.47, N = 17; MK-801/pretesting crossing 29.06, rearing 13.76, N = 17.
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Animal Model:Wistar (male adult, 200-250 g)[5]
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Dosage:30 mg/kg (0, 3, 6, or 9 h post-training); 30 mg/kg (30 min before testing)
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Administration:i.p.; post-training at 0, 3, 6, or 9 h; 30 min before testing
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Result:30 mg/kg injected 0, 3, 6, or 9 h post-training reduced step-down latencies at testing.
Pre-test 30 mg/kg alone did not alter step-down latencies, but reversed the performance deficit induced by post-training 30 mg/kg given at 0, 3, or 6 h, but not at 9 h.
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Animal Model:Wistar (male adult, 200-250 g)[5]
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Dosage:30 mg/kg (immediately post-training); 30 mg/kg (30 min before testing)
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Administration:i.p.; immediately post-training; 30 min before testing
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Result:Post-training 30 mg/kg reduced step-down latencies at testing.
Pre-test 30 mg/kg reversed the performance deficit induced by post-training 30 mg/kg.
Pre-test 30 mg/kg also reversed the performance deficit induced by post-training comparator, demonstrating transfer of comparator-induced state dependency.\nPost-training 30 mg/kg reduced step-down latencies at testing.
Post-training naloxone 2 mg/kg reversed the performance deficit induced by post-training 30 mg/kg.
Pre-test naloxone 1 mg/kg did not reverse the performance deficit induced by post-training 30 mg/kg.
Post-training naloxone reversed the state dependency induced by post-training 30 mg/kg.
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Animal Model:Wistar (male adult, 200-250 g)[5]
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Dosage:10 mg/kg (post-training and pre-test); 10 mg/kg plus 1.5 mg/kg comparator (combination); 1.5 mg/kg plus 10 mg/kg comparator (alternative association)
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Administration:i.p.; immediately post-training; 30 min before testing
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Result:Low-dose 10 mg/kg or comparator 1.5 mg/kg alone was non-effective.
Combined low-dose 10 mg/kg plus comparator 1.5 mg/kg administered post-training impaired performance at testing, and pre-test combined 10 mg/kg plus comparator 1.5 mg/kg reversed the deficit, indicating additive state dependency.
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Animal Model:Wistar (male, 220-260 g)[6]
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Dosage:0.1 mg/kg, 1 mg/kg, and 10 mg/kg
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Administration:i.p.; single injection immediately after training
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Result:At 10 mg/kg, contextual and auditory fear conditioning were impaired.
At 0.1 mg/kg and 1 mg/kg, conditioning was not impaired.
In the novel context without tone, freezing was 13.67% at 0.1 mg/kg, 13.51% at 1 mg/kg, and 11.01% at 10 mg/kg.
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Animal Model:Wistar (male, 220-260 g)[6]
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Dosage:10 mg/kg
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Administration:i.p.; single injection at 0, 60, 180, or 360 min after training
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Result:At 0, 60, or 180 min after training, contextual and auditory fear conditioning were impaired.
At 360 min after training, no impairment was observed.
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Animal Model:Wistar (male, 220-260 g)[6]
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Dosage:0.1 mg/kg
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Administration:i.p.; single injection immediately after training; co-administered with spermidine 100 mg/kg in the opposite flank
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Result:A dose of 0.1 mg/kg, with no effect alone, reversed the facilitatory effect of spermidine on contextual and auditory fear conditioning.
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Animal Model:Swiss albino (male, 25-28 g)[8]
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Dosage:25 μg/mouse
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Administration:i.c.v.; single administration
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Result:Increased tail-flick reaction latency at 20 minutes.
No increase in reaction latency was observed at 40, 60, or 90 minutes.
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Animal Model:Swiss albino (male, 25-28 g)[8]
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Dosage:25 μg/mouse
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Administration:i.c.v.; single administration; 10 minutes before ethanol 1 g/kg i.p.
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Result:Increased reaction latency versus the control group at 20 and 40 minutes.
No increase was observed at 60 or 90 minutes.
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Animal Model:Swiss albino (male, 25-28 g)[8]
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Dosage:25 μg/mouse
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Administration:i.c.v.; once daily on days 1-8; before daily ethanol 2 g/kg i.p. or saline i.p.
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Result:Attenuated development of tolerance to ethanol-induced anti-nociception.
On day 9, reaction latency remained higher than in the ethanol-only group.
In saline-treated mice, tail-flick latencies were 3.00 s on day 1, 3.14 s on day 3, 2.71 s on day 5, 3.14 s on day 7, and 3.00 s on day 9.
Chemical Information
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No. CAS 544-05-8
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Peso molecular 172.24
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Fòrmula C6H16N6
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SMILES
N=C(N)NCCCCNC(=N)N
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Synonyms
ARC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Pureza:
99.98%
Assay:
99.98%
ee.:
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Arcaine Related Classifications
HY-187833 Related Classifications
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