Sigma receptor

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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 - уреди | uredi izvor]

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 - уреди | uredi izvor]

Agonisti[uredi - уреди | uredi izvor]

Antagonisti[uredi - уреди | uredi izvor]

Literatura[uredi - уреди | uredi izvor]

  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. PMC 2596726. PMID 17456670. doi:10.1213/01.ane.0000260267.71185.73. 
  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. PMC 2947205. PMID 19213917. doi:10.1126/science.1166127. 
  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. 
  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. PMC 2080825. PMID 17617400. doi:10.1016/j.ejphar.2007.06.012. 
  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. PMC 2872963. PMID 20100904. doi:10.1124/jpet.109.161398. 
  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

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