α-Chlorohydrin: Review of a Model Posttesticular Antifertility Agent

Lobl, Thomas J.

doi:10.1007/978-94-009-8875-0_11

Cited by 8 publications

(6 citation statements)

References 65 publications

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“…Both -chlorohydrin (see Jones, A.R., 1978Jones, A.R., , 1983Lobi, 1980) and the 6-chloro-6-deoxysugars (see Ford, 1982) have a rapid and reversible antifertility action in male animals. The contraceptive effect is believed to result from the inhibition of glyceraldehyde 3-phosphate dehydrogenase (EC 1.2.1.12) in spermatozoa (Brown-Woodman, Mohri, Mohri, Suter & White, 1978;Ford, Harrison & Waites, 1981).…”

Section: Introductionmentioning

confidence: 99%

The presence of glucose increases the lethal effect of -chlorohydrin on ram and boar spermatozoa in vitro

Ford¹,

Harrison²

1985

Reproduction

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Ram cauda epididymal spermatozoa were incubated for 10 min at 34 degrees C with or without 1.0 mM-RS-alpha-chlorohydrin before (1) 5 mM-D-glucose or (2) 10 mM-L-lactate plus 1 mM pyruvate or (3) 5 mM-D-glucose plus 10 mM-L-lactate plus 1 mM-pyruvate or (4) no substrate was added. Without alpha-chlorohydrin, the motility, the ATP concentration and the energy charge of the spermatozoa were maintained for 240 min by substrate combinations 1-3 but with no added substrate (4) the motility declined after 60 min. All the values decreased dramatically after 10 min in spermatozoa exposed to alpha-chlorohydrin in substrate conditions 1 and 3 (glucose present) but alpha-chlorohydrin had no significant effect in conditions 2 and 4 (no glucose) except after prolonged incubation. In a dose-response experiment glucose-dependent ATP dissipation began to occur with 0.025 mM-RS-alpha-chlorohydrin. A similar effect was seen in boar spermatozoa exposed to 0.1-5.0 mM-alpha-chlorohydrin and 5 mM-D-glucose. With boar spermatozoa the presence of 10 mM-L-lactate and 1 mM-pyruvate as well as glucose prevented the loss of ATP. We conclude that this concerted action of alpha-chlorohydrin and glucose is probably responsible for the contraceptive action of alpha-chlorohydrin and propose that it may depend on 'futile substrate cycling' in the glycolytic pathway.

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Section: Introductionmentioning

confidence: 99%

The presence of glucose increases the lethal effect of -chlorohydrin on ram and boar spermatozoa in vitro

Ford¹,

Harrison²

1985

Reproduction

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“…The first report that a-chlorohydrin [3-chloropropan-l,2-diol (1)] possessed antifertility activity in the male was published by Coppola (1969) and the first major review of its activity was written in 1977 (Jones 1978a). While this article outlines the progress that has been achieved over the period 1977-82, several aspects of the antifertility action of a-chlorohydrin have been included in books (Brooks 1979a; Mann and Lutwak-Mann 1981) and in more general reviews of male contraception and fertility (Gomes 1977;Jackson and Morris 1979;LobI 1980;Waites 1980;Feghali and Feghali 1982).…”

Section: Introductionmentioning

confidence: 99%

Antifertility Actions of a-Chlorohydrin in the Male

Ar¹

1983

Aust. Jnl. Of Bio. Sci.

112

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Non-steroidal chemicals that affect male fertility have been known for over 25 years but only one compound, alpha-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 alpha-chlorohydrin can be neurotoxic, nephrotoxic and, in rats, lead to prolonged or permanent infertility. However, the antifertility response and the toxicity of racemic alpha-chlorohydrin may be due, respectively, to the separate enantiomers. No other antifertility chemical has been investigated to such an extent as alpha-chlorohydrin; this article reviews the progress that has been achieved with alpha-chlorohydrin during the past six years.

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“…The reduction in epididymal sperm motility produced by a-chlorohydrin and all the analogues apart from compound 3 was not unexpected in view of the data that the primary effect of a-chlorohydrin is directed towards the sperm in the epididymis and it produces biochemical changes in the organ (Crabo and Appelgren 1972;BrownWoodman andWhite, 1975, 1976;LobI 1980;Tsang et al 1981;Paz and Homonnai 1982). Low doses of a-chlorohydrin do not affect the weight or ultrastructure of the epididymis (Reijonen et al 1975) and thus the fact that none of the derivatives produced change in epididymal weight was not surprising.…”

Section: Resultsmentioning

confidence: 99%

Antifertility Activity and Toxicity of a-Chlorohydrin Aromatic Ketal Analogues in Male Rats

Brown‐Woodman¹,

White²,

Ridley³

1986

Aust. Jnl. Of Bio. Sci.

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The antifertility activity and toxicity of a-chlorohydrin and seven aromatic ketal derivatives were investigated in male rats. At a dose of 5 mg/kg injected intraperitioneally.each day for 14 days, a-chlorohydrin and the methoxy benzaldehyde derivative (compound 2) produced complete infertility. The benzaldehyde derivative (compound 1) was 89% effective and the other five compounds 71-25% effective. All compounds except the least effective antifertility agent, the methylbenzaldehyde derivative (compound 3), reduced the motility of sperm recovered from the epididymis. None of the compounds caused a decrease in body or testes weight but some increased adrenal weight.

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α-Chlorohydrin: Review of a Model Posttesticular Antifertility Agent

Cited by 8 publications

References 65 publications

The presence of glucose increases the lethal effect of -chlorohydrin on ram and boar spermatozoa in vitro

The presence of glucose increases the lethal effect of -chlorohydrin on ram and boar spermatozoa in vitro

Antifertility Actions of a-Chlorohydrin in the Male

Antifertility Activity and Toxicity of a-Chlorohydrin Aromatic Ketal Analogues in Male Rats

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