Galmic
Galmic is a selective non-peptide GalR1-selective galanin receptor agonist that crosses the blood-brain barrier, with a human Ki of 34.2 μM. Galmic can be used for research on status epilepticus and epilepsy.
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- CAS No.: 762241-24-7
- Formule: C51H60N10O11
- Masse moléculaire:989.08
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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GalR1 34.2 μM (Ki) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Galmic (2.45-9.8 µmol/kg; intraperitoneal injection; once; 15 minutes before formalin injection) inhibits formalin-induced licking behavior in mice in a dose-dependent manner[1].
Galmic (15 mg/kg; intraperitoneal injection; once; 40 minutes before the forced swimming test) increases active behavior in rats in the forced swimming test[1].
Galmic (15 mg/kg; intraperitoneal injection; once; 40 minutes before the open field test) reduces locomotor activity in rats in the open field test[1].
Galmic (systemic administration) effectively inhibits seizures induced by perforant pathway stimulation[2].
Galmic (systemic administration) effectively inhibits Pentylenetetrazole-induced seizures[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, adult)[1]
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Dosage:0.02 nmol (intrahippocampal, 10 min after stimulation);0.1 nmol (intrahippocampal, 10 min after stimulation); 1 nmol (intrahippocampal, 10 min after stimulation); 5 nmol (intrahippocampal, 10 min after stimulation); 5 nmol (intrahippocampal, 60 min after stimulation); 10 nmol (intrahippocampal, 60 min after stimulation); 1 mg/kg (i.p., 10 min after stimulation); 2 mg/kg (i.p., 10 min after stimulation)
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Administration:intrahippocampal once 10 min after stimulation; intrahippocampal once 60 min after stimulation; i.p. once 10 min after stimulation
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Result:At 0.1 nmol, SSSE duration was 1-2 h versus 10-12 h in controls; effects were stronger at 1 and 5 nmol.
At 5 nmol, seizures were abolished within 5-10 min and spikes within 2 h.
During maintenance, 5 and 10 nmol attenuated SSSE; 10 nmol shortened SSSE duration to 4-5 h, time spent in seizures to 20-40 min, and spike duration to under 8 h versus 24 h in controls.
At 2 mg/kg i.p., self-sustaining seizures were attenuated, whereas 1 mg/kg i.p. had no effect.
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Animal Model:C57BL/6 (male, 25-30 g)[1]
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Dosage:2.45 µmol/kg (i.p., 15 min before formalin); 4.9 µmol/kg (i.p., 15 min before formalin); 9.8 µmol/kg (i.p., 15 min before formalin)
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Administration:i.p.; once; 15 min before formalin
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Result:Produced dose-dependent inhibition of both phase 1 and phase 2 flinching.
The ED50 for inhibition of phase 1 was 2.9 µmol/kg (95% CI 2.1-4.1), and for phase 2 was 3.7 µmol/kg (95% CI 2.6-5.2).
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Animal Model:Rats[1]
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Dosage:15 mg/kg
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Administration:i.p.; once; 40 min before forced-swim test
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Result:Increased time spent active by 55% relative to vehicle-treated rats.
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Animal Model:Rats[1]
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Dosage:15 mg/kg
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Administration:i.p.; once; 40 min before open-field test
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Result:Reduced total squares crossed by more than half relative to vehicle-treated rats.
Chemical Information
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CAS No. 762241-24-7
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Masse moléculaire 989.08
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Formule C51H60N10O11
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SMILES
O=C([C@]1(C2=NC(C(N[C@](C)(C3=NC(C(N[C@](C)(C4=NC(C(N1)=O)=C(O4)C)C(NCC5CCCCC5)=O)=O)=C(O3)C)C(N[C@H](C(OC)=O)CCCCN)=O)=O)=C(O2)C)C)NC6C7=CC=CC=C7C8=CC=CC=C86
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Bartfai T, et al. Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests. Proceedings of the National Academy of Sciences of the United States of America. 2004 Jul 13;101(28):10470-5. [Content Brief]
[2]. Mazarati AM, et al. Galanin and galanin receptors in epilepsy. Neuropeptides. 2004 Dec;38(6):331-43. [Content Brief]
[3]. Ceide SC, et al. Synthesis of galmic: a nonpeptide galanin receptor agonist. Proceedings of the National Academy of Sciences of the United States of America. 2004 Nov 30;101(48):16727-32. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Galmic Related Classifications
HY-189079 Related Classifications
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