Synthetic modulators of the complement system. 1. Synthesis and biological activity of 5,5',5"-[1,3,6-naphthalenetriyltris(sulfonylimino)]tris[1,3-benzenedisulfonate] hexasodium salt

Conrow, R. B.; Bauman, Norman; Brockman, John A.; Bernstein, Seymour

doi:10.1021/jm00177a006

Cited by 8 publications

(3 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…These results indicate that 2-hydroxystilbamidine [12,13], which inhibits Clrand Cls enzymes and interacts with the B-determinant of C3 [13], reduces C3 fixation at the site of Arthus reaction. Suramin [7][8][9][10][11] which does not inhibit Clr and Cls (unpub lished observations) but inhibits interactions between EA and C1, EAC1 and C4, EAC142 and C3-C9, EAC 1-7 and C8 and reacts irre versibly with bound C3 preventing its de struction by C3b inactivator, was compara tively less effective.…”

Section: Discussionmentioning

confidence: 76%

“…To inhibit complement activity in un diluted serum, usually very high concentra tions of strong inhibitors are needed. In a report by Conrow et al [12] intraperitoneal administration of 200 mg/kg suramin to guinea pigs weighing 300 g caused only 44% inhibition in undiluted serum. Thus, under our experimental conditions drug levels in serum could not have fallen within the range of concentration which are 100% effective in vitro in blood.…”

Section: Effects Of Complement Inhibitors On Deposition Of Complementmentioning

confidence: 99%

“…More recently, suppression of development of EAE and suppression of hu man vasculitis by the complement inhibitors suramin [6] and chlorpromazine [7], respec tively, has been shown. Here we show that certain low molecular weight complement in hibitors, namely suramin [8][9][10][11][12], 2-hydroxystilbamidine [13,14], chlorpromazine [15] and chlorophenothiazine sulphonate [ 16] can strongly suppress complement-mediated vas cular injury seen in the Arthus reaction. of saline and incomplete Freund's adjuvant was given.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Suppression of Complement-Mediated Vascular Injury at Arthus Reaction Sites by Complement Inhibitors

Ss¹,

Kp²,

Kammeijer³

et al. 1986

Complement

View full text Add to dashboard Cite

Certain complement inhibitors, namely chlorpromazine, suramin, 2-hydroxystilbamidine and chlorophenothiazine sulphonate were tested for their ability to suppress complement deposition and vascular injury at the site of an Arthus reaction. Deposition of complement was suppressed in the order 2-hydroxystilbamidine > suramin > chlorpromazine. All the above mentioned four compounds strongly protected vascular injury as observed by electron microscopic studies. At Arthus reaction sites prepared without drug treatment venules ranged from normal to severely altered and damaged. Discontinuities in endothelial linings varied from small to longer stretches. In the latter situation remaining endothelial cells were degenerated and endothelial remnants did not have an intact basal lamina. After treatment with the above complement inhibitors, at arthus reaction sites some venules appeared normal, whereas others were altered but in all cases the endothelium and its basal lamina remained intact.

show abstract