Background: The purpose of this study was to investigate the fertility-regulating potential of the compound 2-(2″-chloroacetamidobenzyl)-3-(3′-indolyl) quinoline in male rats. Study Design: Rats of proven fertility were treated with the compound by oral gavage for 1 to 8 consecutive weeks. Functional fertility, testicular, epididymal and seminal vesicular weight, epididymal sperm count and spermatogenesis were quantitated. Reproductive hormones and some biochemical parameters were measured. Results: Functional fertility was reduced significantly as revealed by a fall in fertility and pregnancy rate. The weight of the reproductive organs was reduced significantly. A reduction of sperm count and number of different types of testicular cells was observed. The treatment with the compound resulted in decline of testosterone and an increase of FSH hormone levels. The compound effectively reduced testicular protein, glycogen and epididymal glyceryl phosphorylcholine. Increase in testicular alkaline phosphatase and cholesterol was also observed. Fertility and other effects were regained gradually after cessation of treatment. Conclusion: The results revealed from the study indicate that the compound has reversible antifertility activity and can be explored as male contraceptive agent. © 2008 Elsevier Inc. All rights reserved.