Neuropeptide receptor positive allosteric modulation in epilepsy: Galanin modulation revealed

Proceedings of the National Academy of Sciences of the United States of America

Volumn 107, Issue 34, 2010, Pages 14943-14944

  Hoyer, Daniel ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ANGIOTENSIN; CALCITONIN GENE RELATED PEPTIDE; CORTICOTROPIN RELEASING FACTOR; ENDOTHELIN; G PROTEIN COUPLED RECEPTOR; GALANIN; GHRELIN RECEPTOR; GLUCAGON LIKE PEPTIDE; NEUROPEPTIDE RECEPTOR; NEUROPEPTIDE Y; OREXIN; SOMATOSTATIN; TACHYKININ; GALANIN RECEPTOR 2; LIGAND;

ALLOSTERISM; BIOAVAILABILITY; CELL LINE; EPILEPSY; EPILEPTOGENESIS; HIPPOCAMPUS; HUMAN; NONHUMAN; NOTE; PAIN; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN EXPRESSION; SEIZURE; ANIMAL; DRUG POTENTIATION; METABOLISM; MOLECULAR WEIGHT;

ALLOSTERIC REGULATION; ANIMALS; EPILEPSY; GALANIN; HUMANS; LIGANDS; MOLECULAR WEIGHT; RECEPTOR, GALANIN, TYPE 2; RECEPTORS, NEUROPEPTIDE;

EID: 77957013648     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1010365107     Document Type: Note

References (18)

1. Hökfelt T, Bartfai T, Bloom F (2003) Neuropeptides: Opportunities for drug discovery. Lancet Neurol 2:463-472.
2. Lu X, et al. (2010) GalR2 positive allosteric modulator exhibits anticonvulsant effects in animal models. Proc Natl Acad Sci USA 107:15229-15234.
3. Vezzani A, et al. (1994) Enhanced neuropeptide Y release in the hippocampus is associated with chronic seizure susceptibility in kainic acid treated rats. Brain Res 660:138-143.
4. Vezzani A, Hoyer D (1999) Brain somatostatin: A candidate inhibitory role in seizures and epileptogenesis. Eur J Neurosci 11:3767-3776. (Pubitemid 29537557)
5. Noè F, et al. (2008) Neuropeptide Y gene therapy decreases chronic spontaneous seizures in a rat model of temporal lobe epilepsy. Brain 131:1506-1515.
6. May LT, Leach K, Sexton PM, Christopoulos A (2007) Allosteric modulation of G protein-coupled receptors. Annu Rev Pharmacol Toxicol 47:1-51.
7. Holst B, Brandt E, Bach A, Heding A, Schwartz TW (2005) Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol 19:2400-2411.
8. Knudsen LB, et al. (2007) Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc Natl Acad Sci USA 104:937-942.
9. Conn PJ, Christopoulos A, Lindsley CW (2009) Allosteric modulators of GPCRs: A novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 8:41-54.
10. Berry-Kravis E, et al. (2009) A pilot open label, single dose trial of fenobam in adults with fragile X syndrome. J Med Genet 46:266-271.
11. Fallarino F, et al. (2010) Metabotropic glutamate receptor-4 modulates adaptive immunity and restrains neuroinflammation. Nat Med 16:897-902.
12. Fisone G, et al. (1987) Galanin inhibits acetylcholine release in the ventral hippocampus of the rat: Histochemical, autoradiographic, in vivo, and in vitro studies. Proc Natl Acad Sci USA 84:7339-7343.
13. Fisone G, et al. (1989) N-terminal galanin-(1-16) fragment is an agonist at the hippocampal galanin receptor. Proc Natl Acad Sci USA 86:9588-9591.
14. Bartfai T, et al. (1991) M-15: High-affinity chimeric peptide that blocks the neuronal actions of galanin in the hippocampus, locus coeruleus, and spinal cord. Proc Natl Acad Sci USA 88:10961-10965.
15. Bartfai T, et al. (2004) Galmic, a nonpeptide galanin receptor agonist, affects behaviors in seizure, pain, and forced-swim tests. Proc Natl Acad Sci USA 101:10470-10475.
16. Crawley JN, Robinson JK, Langel U, Bartfai T (1993) Galanin receptor antagonists M40 and C7 block galanin-induced feeding. Brain Res 600:268-272. (Pubitemid 23035626)
17. Sollenberg U, Bartfai T, Langel U (2005) Galnon - a low-molecular weight ligand of the galanin receptors. Neuropeptides 39:161-163.
18. White HS, et al. (2009) Developing novel antiepileptic drugs: Characterization of NAX 5055, a systemically-active galanin analog, in epilepsy models. Neurotherapeutics 6:372-380.