Chemistry:SDZ-GLC-756

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SDZ-GLC-756 is a mixed-action dopaminergic drug that has been proposed for use in the treatment of eye diseases associated with high intraocular pressure. It is referred to as GLC756 in modern sources.[1]

Pharmacology

GLC756 acts primarily as a dopaminergic, serotonergic, and adrenergic agent with a broad spectrum of action; the reduction in TNF-alpha levels induced by GLC756 is achieved through its antagonistic effect on α2-adrenergic receptors and its agonistic effect on β2 adrenergiс receptors. In addition, it also exhibits antagonism toward the dopamine receptor D1 and an agonistic effect on the dopamine receptor D2; it has also been shown to bind to α1-adrenergic and β1-adrenergic receptors, to dopamine receptors D4, and to numerous subtypes of 5-hydroxytryptamine receptors, such as 5-HT1A, 5-HT2C, 5-HT1D, and 5-HT2A.[1][2][3][4][5] GLC756 has been described in the literature as an inhibitor of leukotriene C4 release and has also been shown to significantly increase cellular cAMP levels.[6][7]

References

  1. ↑ 1.0 1.1 "GLC756 decreases TNF-alpha via an alpha2 and beta2 adrenoceptor related mechanism". Experimental Eye Research 83 (5): 1246–1251. November 2006. doi:10.1016/j.exer.2006.07.001. PMID 16938291. 
  2. ↑ "Effects of antiglaucoma drugs GLC756, a novel dopamine D2 agonist and D1 antagonist, and timolol on endotoxin-induced TNF-alpha release in serum of rats". European Journal of Ophthalmology 16 (3): 401–406. 2006. doi:10.1177/112067210601600307. PMID 16761241. 
  3. ↑ "Effect of GLC756, a novel mixed dopamine D1 receptor antagonist and dopamine D2 receptor agonist, on TNF-alpha release in vitro from activated rat mast cells". Experimental Eye Research 83 (6): 1335–1339. December 2006. doi:10.1016/j.exer.2006.07.008. PMID 16965772. 
  4. ↑ "Effects of dopamine D-1 and D-2 receptors on intraocular pressure in conscious rabbits". Journal of Neural Transmission (Vienna) 104 (2–3): 111–123. 1997. doi:10.1007/BF01273174. PMID 9203075. 
  5. ↑ "Topical SDZ GLC-756, a novel dopamine D-1 antagonist and D-2 agonist, lowers intraocular pressure in conscious rabbits". Japanese Journal of Ophthalmology 40 (2): 167–173. 1996. PMID 8876383. 
  6. ↑ "Effects of latanoprost, timolol and GLC756, a novel dopamine D(2) agonist and D(1) antagonist on LTC(4) release after rat mast cell activation". Clinical & Experimental Ophthalmology 35 (7): 645–650. 2007. doi:10.1111/j.1442-9071.2007.01560.x. PMID 17894685. 
  7. ↑ "Antiglaucoma drug GLC756 and its effect on cellular cAMP and tumor necrosis factor alpha release in vitro of activated human monocytic leukemia cells". Japanese Journal of Ophthalmology 53 (2): 159–163. March 2009. doi:10.1007/s10384-008-0625-8. PMID 19333701. 



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