SR-48692

SR-48692
(IUPAC) ime
	2-([1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carbonyl]amino)admantane-2-carboxylic acid
Klinički podaci
Identifikatori
CAS broj	146362-70-1
ATC kod	?
PubChem	119192
Hemijski podaci
Formula	C32H31ClN4O5
Mol. masa	587.064
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C32H31ClN4O5/c1-41-27-4-3-5-28(42-2)29(27)26-16-24(36-37(26)25-8-9-34-23-15-21(33)6-7-22(23)25)30(38)35-32(31(39)40)19-11-17-10-18(13-19)14-20(32)12-17/h3-9,15-20H,10-14H2,1-2H3,(H,35,38)(H,39,40) ; Key: DYLJVOXRWLXDIG-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

SR-48692 je lek koji je selektivni, nepeptidni antagonist neurotenzinskog receptora NTS₁. On je bio prvi nepeptidni antagonist razvijen za ovaj receptor.^[3]^[4] SR-48692 se koristi u naučnim istraživanjima za izučavanje interakcija između neurotenzina i drugih neurotransmitera u mozgu.^[5]^[6]^[7]^[8]^[9]^[10] On proizvodi anksiolitske, antiadiktivne i efekte ograničavanja memorije u životinjskim studijama.^[11]^[12]^[13]^[14]

Reference uredi

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Gully D, Canton M, Boigegrain R, Jeanjean F, Molimard JC, Poncelet M, Gueudet C, Heaulme M, Leyris R, Brouard A (January 1993). „Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor”. Proceedings of the National Academy of Sciences of the United States of America 90 (1): 65–9. DOI:10.1073/pnas.90.1.65. PMC 45600. PMID 8380498.
↑ Gully D, Jeanjean F, Poncelet M, Steinberg R, Soubrié P, Le Fur G, Maffrand JP (1995). „Neuropharmacological profile of non-peptide neurotensin antagonists”. Fundamental & Clinical Pharmacology 9 (6): 513–21. DOI:10.1111/j.1472-8206.1995.tb00528.x. PMID 8808171.
↑ Rostene W, Azzi M, Boudin H, Lepee I, Souaze F, Mendez-Ubach M, Betancur C, Gully D (April 1997). „Use of nonpeptide antagonists to explore the physiological roles of neurotensin. Focus on brain neurotensin/dopamine interactions”. Annals of the New York Academy of Sciences 814: 125–41. PMID 9160965.
↑ Jolas T, Aghajanian GK (August 1997). „Neurotensin and the serotonergic system”. Progress in Neurobiology 52 (6): 455–68. DOI:10.1016/S0301-0082(97)00025-7. PMID 9316156.
↑ Dobner PR, Deutch AY, Fadel J (June 2003). „Neurotensin: dual roles in psychostimulant and antipsychotic drug responses”. Life Sciences 73 (6): 801–11. DOI:10.1016/S0024-3205(03)00411-9. PMID 12801600.
↑ Chen L, Yung KK, Yung WH (September 2006). „Neurotensin selectively facilitates glutamatergic transmission in globus pallidus”. Neuroscience 141 (4): 1871–8. DOI:10.1016/j.neuroscience.2006.05.049. PMID 16814931.
↑ Petkova-Kirova P, Rakovska A, Della Corte L, Zaekova G, Radomirov R, Mayer A (September 2008). „Neurotensin modulation of acetylcholine, GABA, and aspartate release from rat prefrontal cortex studied in vivo with microdialysis”. Brain Research Bulletin 77 (2-3): 129–35. DOI:10.1016/j.brainresbull.2008.04.003. PMID 18721670.
↑ Petkova-Kirova P, Rakovska A, Zaekova G, Ballini C, Corte LD, Radomirov R, Vágvölgyi A (December 2008). „Stimulation by neurotensin of dopamine and 5-hydroxytryptamine (5-HT) release from rat prefrontal cortex: possible role of NTR1 receptors in neuropsychiatric disorders”. Neurochemistry International 53 (6-8): 355–61. DOI:10.1016/j.neuint.2008.08.010. PMID 18835308.
↑ Griebel G, Moindrot N, Aliaga C, Simiand J, Soubrié P (December 2001). „Characterization of the profile of neurokinin-2 and neurotensin receptor antagonists in the mouse defense test battery”. Neuroscience and Biobehavioral Reviews 25 (7-8): 619–26. DOI:10.1016/S0149-7634(01)00045-8. PMID 11801287.
↑ Tirado-Santiago G, Lázaro-Muñoz G, Rodríguez-González V, Maldonado-Vlaar CS (October 2006). „Microinfusions of neurotensin antagonist SR 48692 within the nucleus accumbens core impair spatial learning in rats”. Behavioral Neuroscience 120 (5): 1093–102. DOI:10.1037/0735-7044.120.5.1093. PMID 17014260.
↑ Felszeghy K, Espinosa JM, Scarna H, Bérod A, Rostène W, Pélaprat D (December 2007). „Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology 32 (12): 2601–10. DOI:10.1038/sj.npp.1301382. PMID 17356568.
↑ Lévesque K, Lamarche C, Rompré PP (October 2008). „Evidence for a role of endogenous neurotensin in the development of sensitization to the locomotor stimulant effect of morphine”. European Journal of Pharmacology 594 (1-3): 132–8. DOI:10.1016/j.ejphar.2008.07.048. PMID 18706409.

Spoljašnje veze uredi

	Portal Medicina
	Portal Hemija

Šablon:Neuropeptidni ligandi

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[pmid8380498-3] Gully D, Canton M, Boigegrain R, Jeanjean F, Molimard JC, Poncelet M, Gueudet C, Heaulme M, Leyris R, Brouard A (January 1993). „Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor”. Proceedings of the National Academy of Sciences of the United States of America 90 (1): 65–9. DOI:10.1073/pnas.90.1.65. PMC 45600. PMID 8380498.

[pmid8808171-4] Gully D, Jeanjean F, Poncelet M, Steinberg R, Soubrié P, Le Fur G, Maffrand JP (1995). „Neuropharmacological profile of non-peptide neurotensin antagonists”. Fundamental & Clinical Pharmacology 9 (6): 513–21. DOI:10.1111/j.1472-8206.1995.tb00528.x. PMID 8808171.

[pmid9160965-5] Rostene W, Azzi M, Boudin H, Lepee I, Souaze F, Mendez-Ubach M, Betancur C, Gully D (April 1997). „Use of nonpeptide antagonists to explore the physiological roles of neurotensin. Focus on brain neurotensin/dopamine interactions”. Annals of the New York Academy of Sciences 814: 125–41. PMID 9160965.

[pmid9316156-6] Jolas T, Aghajanian GK (August 1997). „Neurotensin and the serotonergic system”. Progress in Neurobiology 52 (6): 455–68. DOI:10.1016/S0301-0082(97)00025-7. PMID 9316156.

[pmid12801600-7] Dobner PR, Deutch AY, Fadel J (June 2003). „Neurotensin: dual roles in psychostimulant and antipsychotic drug responses”. Life Sciences 73 (6): 801–11. DOI:10.1016/S0024-3205(03)00411-9. PMID 12801600.

[pmid16814931-8] Chen L, Yung KK, Yung WH (September 2006). „Neurotensin selectively facilitates glutamatergic transmission in globus pallidus”. Neuroscience 141 (4): 1871–8. DOI:10.1016/j.neuroscience.2006.05.049. PMID 16814931.

[pmid18721670-9] Petkova-Kirova P, Rakovska A, Della Corte L, Zaekova G, Radomirov R, Mayer A (September 2008). „Neurotensin modulation of acetylcholine, GABA, and aspartate release from rat prefrontal cortex studied in vivo with microdialysis”. Brain Research Bulletin 77 (2-3): 129–35. DOI:10.1016/j.brainresbull.2008.04.003. PMID 18721670.

[pmid18835308-10] Petkova-Kirova P, Rakovska A, Zaekova G, Ballini C, Corte LD, Radomirov R, Vágvölgyi A (December 2008). „Stimulation by neurotensin of dopamine and 5-hydroxytryptamine (5-HT) release from rat prefrontal cortex: possible role of NTR1 receptors in neuropsychiatric disorders”. Neurochemistry International 53 (6-8): 355–61. DOI:10.1016/j.neuint.2008.08.010. PMID 18835308.

[pmid11801287-11] Griebel G, Moindrot N, Aliaga C, Simiand J, Soubrié P (December 2001). „Characterization of the profile of neurokinin-2 and neurotensin receptor antagonists in the mouse defense test battery”. Neuroscience and Biobehavioral Reviews 25 (7-8): 619–26. DOI:10.1016/S0149-7634(01)00045-8. PMID 11801287.

[pmid17014260-12] Tirado-Santiago G, Lázaro-Muñoz G, Rodríguez-González V, Maldonado-Vlaar CS (October 2006). „Microinfusions of neurotensin antagonist SR 48692 within the nucleus accumbens core impair spatial learning in rats”. Behavioral Neuroscience 120 (5): 1093–102. DOI:10.1037/0735-7044.120.5.1093. PMID 17014260.

[pmid17356568-13] Felszeghy K, Espinosa JM, Scarna H, Bérod A, Rostène W, Pélaprat D (December 2007). „Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference”. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology 32 (12): 2601–10. DOI:10.1038/sj.npp.1301382. PMID 17356568.

[pmid18706409-14] Lévesque K, Lamarche C, Rompré PP (October 2008). „Evidence for a role of endogenous neurotensin in the development of sensitization to the locomotor stimulant effect of morphine”. European Journal of Pharmacology 594 (1-3): 132–8. DOI:10.1016/j.ejphar.2008.07.048. PMID 18706409.

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]

[12]

[13]

[14]

[1]

[2]