Sigma receptor

Izvor: Wikipedija
Prijeđi na navigaciju Prijeđi na pretragu
Šematski prikaz σ receptora

Sigma receptori σ1 i σ2 vezuju ligande kao što su 4-PPBP,[1] SA 4503, ditolilgvanidin, dimetiltriptamin[2] i siramesin.[3]

Klasifikacija[uredi | uredi kod]

Za sigma receptori se nekad mislilo da su tip opioidnih receptora, zato što d stereoizomeri benzomorfanske klase opioidnih lekova ne deluju na μ, κ, i δ receptore, a umanjuju kašalj. Međutim, rezultati farmakoloških testiranja su pokazali da se sigma receptori aktiviraju lekovima koji su potpuno nevezani sa opioidima, i da je njihova funkcija nije srodna sa funkcijom opioidnih receptora. Na primer, fenciklidin (PCP) i antipsihotik haloperidol mogu da interaguju sa ovim receptorom. Ova dva leka nemaju hemijske sličnosti sa opioidima.

Kad je σ1 receptor bio izolovan i kloniran, utvrđeno je da nema strukturne sličnosti sa opioidnim receptora. Iz tog razloga je on označen kao zasebna klasa receptora.

Ligandis[uredi | uredi kod]

Agonisti[uredi | uredi kod]

Antagonisti[uredi | uredi kod]

Literatura[uredi | uredi kod]

  1. Yang S, Bhardwaj A, Cheng J, Alkayed NJ, Hurn PD, Kirsch JR (2007). „Sigma receptor agonists provide neuroprotection in vitro by preserving bcl-2”. Anesth. Analg. 104 (5): 1179–84, tables of contents. DOI:10.1213/01.ane.0000260267.71185.73. PMC 2596726. PMID 17456670. 
  2. Fontanilla D, Johannessen M, Hajipour A, Cozzi N, Jackson M, Ruoho A (2009). „The Hallucinogen N,N-Dimethyltryptamine (DMT) Is an Endogenous Sigma-1 Receptor Regulator”. Science 323 (5916): 934–937. DOI:10.1126/science.1166127. PMC 2947205. PMID 19213917. 
  3. Skuza G, Rogóz Z (2006). „The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats”. J. Physiol. Pharmacol. 57 (2): 217–29. PMID 16845227. 
  4. Calabrese JR, Suppes T, Bowden CL, et al. (November 2000). „A double-blind, placebo-controlled, prophylaxis study of lamotrigine in rapid-cycling bipolar disorder. Lamictal 614 Study Group”. The Journal of Clinical Psychiatry 61 (11): 841–50. PMID 11105737. Pristupljeno 2011-04-24. 
  5. Ng F, Hallam K, Lucas N, Berk M (August 2007). „The role of lamotrigine in the management of bipolar disorder”. Neuropsychiatric Disease and Treatment 3 (4): 463–74. PMC 2655087. PMID 19300575. Pristupljeno 2011-04-24. 
  6. Maeda DY, Williams W, Bowen WD, Coop A (January 2000). „A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays”. Bioorganic & Medicinal Chemistry Letters 10 (1): 17–8. PMID 10636233. 
  7. Wu HE, Hong JS, Tseng LF (October 2007). „Stereoselective action of (+)-morphine over (-)-morphine in attenuating the (-)-morphine-produced antinociception via the naloxone-sensitive sigma receptor in the mouse”. European Journal of Pharmacology 571 (2-3): 145–51. DOI:10.1016/j.ejphar.2007.06.012. PMC 2080825. PMID 17617400. 
  8. Xu YT, Kaushal N, Shaikh J, et al. (May 2010). „A novel substituted piperazine, CM156, attenuates the stimulant and toxic effects of cocaine in mice”. J. Pharmacol. Exp. Ther. 333 (2): 491–500. DOI:10.1124/jpet.109.161398. PMC 2872963. PMID 20100904. [mrtav link]
  9. Hashimoto, K (2009). „Sigma-1 Receptors and Selective Serotonin Reuptake Inhibitors: Clinical Implications of their Relationship”. Central Nervous System Agents in Medicinal Chemistry 2009 (Sept): 197–204.  [1]PDF

Spoljašnje veze[uredi | uredi kod]