Topic
Alpha-Chlorohydrin
About: Alpha-Chlorohydrin is a research topic. Over the lifetime, 67 publications have been published within this topic receiving 1760 citations.
Papers published on a yearly basis
Papers
TL;DR: Compound acceptance and potency, route and length of administration, and biological effectiveness make U-5897 and the concept of a male chemosterilant worthy of practical consideration.
Abstract: Summary. U-5897 (3-chloro-1,2-propanediol) is an effective male rat chemosterilant. Sterility results from a lesion in the initial segment of the caput epididymidis. Minimal amounts required to develop lesions consistently are daily oral doses of 35 mg/kg body weight or one 45 mg/kg dose. The immediate consequences of the lesion are sperm blockage in ductuli efferentes and testicular swelling. Fluid accumulation in the testis causes pressure degeneration of the germinal epithelium. Testicular damage does not include morphological or functional (coitus, vaginal plugs, limited spermatogenesis) impairment of Leydig cells. U-5897 is thought to cause local ischaemia, with resultant epithelial desquamation which blocks the caput epididymidis. This is followed by the formation of spermatocoeles, sperm granulomata, and fibrosis. Males made sterile with such a lesion had normal libido with seventy-one matings out of seventy-seven opportunities (92%) over a 64-day period. Adult rats given a single oral dose of 90 to 100 mg/kg of U-5897 still had lesions blocking sperm passage when killed at 3-month intervals over at least 12 months. Although sterile, they continued to mateand enjoyed good general health. Testes were small due to many non-functional seminiferous tubules but spermatogenesis continued in a few tubules. Compound acceptance and potency, route and length of administration, and biological effectiveness make U-5897 and the concept of a male chemosterilant worthy of practical consideration.
129 citations
113 citations
TL;DR: In this article, α-Chlorohydrin produced reversible sterility in male rats and the minimally effective oral dose was 5 mg/kg/day × 14 which was 5 times lower than the anti-spermatogenic dose.
102 citations
TL;DR: The initial and primary contraceptive effect seems to be directly on spermatozoa within the cauda epididymis of the rat, and elucidation of the mechanism of action is clearly important in order to develop less toxic yet more active antifertility analogues.
Abstract: THE potential of α-chlorohydrin (3-chloro-1,2-propanediol; Fig. 1a) as an orally active reversible male antifertility agent has been demonstrated in the rat1,2, ram3 and boar4. Adverse side-effects, however, particularly in the monkey5, have precluded human trials and for this reason, elucidation of the mechanism of action6,7 of α-chlorohydrin is clearly important in order to develop less toxic yet more active antifertility analogues. Although high doses obstruct the lumen of the caput epididymis of the rat2, the initial and primary contraceptive effect seems to be directly on spermatozoa within the cauda epididymis8–11.
100 citations
TL;DR: This article reviews the progress that has been achieved with oc-chlorohydrin during the past six years and investigates the antifertility response and the toxicity of racemic oC- chlorohydrin may be due, respectively, to the separate enantiomers.
Abstract: Non-steroidal chemicals that affect male fertility have been known for over 25 years but only one compound, oc-chlorohydrin, possesses most of the attributes of an ideal male contraceptive. In the male rat, for example, continuous daily oral administration of low doses produces an almost immediate and continuous antifertility response that ceases when treatment is withdrawn. Such a dose regime does not interfere with libido, is apparently not toxic and the action is specific towards mature sperm. Furthermore, the action of the compound is species-specific: it is effective in the rat, ram, boar, guinea pig, hamster,rhesus monkey and upon ejaculated human sperm but it is ineffective in the mouse and the rabbit. High doses of oc-chlorohydrin can be neurotoxic, nephrotoxic and, in rats, lead to prolonged or permanent infertility. However, the antifertility response and the toxicity of racemic oc-chlorohydrin may be due, respectively, to the separate enantiomers. No other antifertility chemical has been investigated to such an extent as oc-chlorohydrin; this article reviews the progress that has been achieved with oc-chlorohydrin during the past six years.
97 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2018 | 1 |
| 2017 | 1 |
| 2016 | 2 |
| 2015 | 1 |
| 2014 | 1 |
| 2011 | 2 |