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
Identifikatori
CAS broj	146362-70-1^Y
PubChem	CID 119192
IUPHAR/BPS	1582
Hemijski podaci
Formula	C₃₂H₃₁ClN₄O₅
Molarna masa	587.064
SMILES c7cc3c(cc7Cl)nccc3-n4nc(cc4-c1c(OC)cccc1OC)C(=O)NC2(C(O)=O)C5CC(C6)CC2CC6C5

SR-48692 je lek koji je selektivni, nepeptidni antagonist neurotenzinskog receptora NTS₁. On je bio prvi nepeptidni antagonist razvijen za ovaj receptor.^[1]^[2] SR-48692 se koristi u naučnim istraživanjima za izučavanje interakcija između neurotenzina i drugih neurotransmitera u mozgu.^[3]^[4]^[5]^[6]^[7]^[8] On proizvodi anksiolitske, antiadiktivne i efekte ograničavanja memorije u životinjskim studijama.^[9]^[10]^[11]^[12]

Reference

^ Gully D, Canton M, Boigegrain R, Jeanjean F, Molimard JC, Poncelet M, Gueudet C, Heaulme M, Leyris R, Brouard A (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. PMC 45600 . PMID 8380498. doi:10.1073/pnas.90.1.65.
^ 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. PMID 8808171. doi:10.1111/j.1472-8206.1995.tb00528.x.
^ Rostene W, Azzi M, Boudin H, Lepee I, Souaze F, Mendez-Ubach M, Betancur C, Gully D (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 (1997). „Neurotensin and the serotonergic system”. Progress in Neurobiology. 52 (6): 455—68. PMID 9316156. doi:10.1016/S0301-0082(97)00025-7.
^ Dobner PR, Deutch AY, Fadel J (2003). „Neurotensin: dual roles in psychostimulant and antipsychotic drug responses”. Life Sciences. 73 (6): 801—11. PMID 12801600. doi:10.1016/S0024-3205(03)00411-9.
^ Chen L, Yung KK, Yung WH (2006). „Neurotensin selectively facilitates glutamatergic transmission in globus pallidus”. Neuroscience. 141 (4): 1871—8. PMID 16814931. doi:10.1016/j.neuroscience.2006.05.049.
^ Petkova-Kirova P, Rakovska A, Della Corte L, Zaekova G, Radomirov R, Mayer A (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. PMID 18721670. doi:10.1016/j.brainresbull.2008.04.003.
^ Petkova-Kirova P, Rakovska A, Zaekova G, Ballini C, Corte LD, Radomirov R, Vágvölgyi A (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. PMID 18835308. doi:10.1016/j.neuint.2008.08.010.
^ Griebel G, Moindrot N, Aliaga C, Simiand J, Soubrié P (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. PMID 11801287. doi:10.1016/S0149-7634(01)00045-8.
^ Tirado-Santiago G, Lázaro-Muñoz G, Rodríguez-González V, Maldonado-Vlaar CS (2006). „Microinfusions of neurotensin antagonist SR 48692 within the nucleus accumbens core impair spatial learning in rats”. Behavioral Neuroscience. 120 (5): 1093—102. PMID 17014260. doi:10.1037/0735-7044.120.5.1093.
^ Felszeghy K, Espinosa JM, Scarna H, Bérod A, Rostène W, Pélaprat D (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. PMID 17356568. doi:10.1038/sj.npp.1301382.
^ Lévesque K, Lamarche C, Rompré PP (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. PMID 18706409. doi:10.1016/j.ejphar.2008.07.048.

Spoljašnje veze

Neuropeptidni ligandi

Holecistokinin

CCK_A	Agonisti: Holecistokinin • CCK-4 Antagonisti: Asperlicin • Proglumid • Lorglumid • Devazepid • Deksloksiglumid
CCK_B	Agonisti: Holecistokinin • CCK-4 • Gastrin Antagonisti: Proglumid • CI-988

CRH

CRF₁	Agonisti: Kortikotropin-oslobađajuči hormon Antagonisti: Antalarmin • CP-154,526 • Peksacerfont
CRF₂	Agonisti: Kortikotropin-oslobađajuči hormon

Galanin

GAL₁	Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL₂	Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL₃	Agonisti: Galanin • Galmic • Galnon

Grelin

Agonisti: Grelin • Kapromorelin • MK-677 • Sermorelin • SM-130,686 • Tabimorelin

MCH

MCH₁	Agonisti: Melanin-koncentrirajući hormon Antagonisti: ATC-0175 • GW-803,430 • NGD-4715 • SNAP-7941 • SNAP-94847
MCH₂	Agonisti: Melanin-koncentrirajući hormon

Melanokortin

MC₁	Agonisti: alfa-MSH • Afamelanotid • Bremelanotid • Melanotan II Antagonisti: Agouti signalni peptid
MC₂	Agonisti: ACTH • Kosintropin • Tetrakosaktid
MC₃	Agonisti: alfa-MSH • Bremelanotid • Melanotan II
MC₄	Agonisti: alfa-MSH • Bremelanotid • Melanotan II • THIQ Antagonisti: Agutiju srodni peptid
MC₅	Agonisti: alfa-MSH • Melanotan II

Neuropeptid S

Agonisti: Neuropeptid S
Antagonisti: SHA-68

Neuropeptid Y

Y₁	Agonisti: Neuropeptid Y • Peptid YY Antagonisti: BIBP-3226
Y₂	Agonisti: Neuropeptid Y • Peptid YY Antagonisti: BIIE-0246
Y₄	Agonisti: Neuropeptid Y • Pankreasni polipeptid • Peptid YY Antagonisti: UR-AK49
Y₅	Agonisti: Neuropeptid Y • Peptid YY Antagonisti: Lu AA-33810

Neurotenzin

NTS₁	Agonisti: Neurotenzin • Neuromedin N Antagonisti: SR-48692 • SR-142,948
NTS₂	Agonisti: Neurotenzin Antagonisti: Levokabastin • SR-142,948

Opioid

vidi Opioidi

Oreksin

OX₁	Agonisti: Oreksin-A Antagonisti: Almoreksant • SB-334,867 • SB-408,124 • SB-649,868
OX₂	Agonisti: Oreksin-A Antagonisti: Almoreksant • SB-649,868 • TCS-OX2-29

Oksitocin

Agonisti: Karbetocin • Demoksitocin • Oksitocin • WAY-267,464
Antagonisti: Atosiban • L-371,257 • L-368,899

Tahikinin

NK₁	Agonisti: Supstanca P Antagonisti: Aprepitant • Befetupitant • Kasopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant
NK₂	Agonisti: Neurokinin A Antagonisti: GR-159897 • Ibodutant • Saredutant
NK₃	Agonisti: Neurokinin B Antagonisti: Osanetant • Talnetant

Vazopresin

V_1A	Agonisti: Dezmopresin • Felipresin • Ornipresin • Terlipresin • Vazopresin Antagonisti: Konivaptan • Demeklociklin • Relkovaptan
V_1B	Agonisti: Felipresin • Ornipresin • Terlipresin • Vazopresin Antagonisti: Demeklociklin • Nelivaptan
V₂	Agonisti: Dezmopresin • Ornipresin • Vazopresin Antagonisti: Konivaptan • Demeklociklin • Liksivaptan • Mozavaptan • Satavaptan • Tolvaptan