A comparative study of serum and testicular concentrations of af 1312/TS (or 1-[(4-chlorophenyl)methyl] 1H-indazole-3-carboxylic acid) and diclondazolic acid (or 1-[(2,4-dichlorophenyl)methyl)]-1H-indazole-3-carboxylic acid) in rats

Catanese, B; Cioli, V.; Martino, C. De; Silvestrini, Bruno

doi:10.1016/s0031-6989(78)80020-4

Cited by 9 publications

(7 citation statements)

References 3 publications

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“…This finding confirms the data of Coulston et al, who reported that 50 mg/kg/day for 5 days resulted in reduced testicular weights in rats [4]. The minimum oral antispermatogenic dose (MED) of DICA has been reported to be 35-56 mg/kg [3, 111 with a testicular drug concentration of 4 pgig tissue at the MED [2]. The serum and testicular absorption profile was similar to that seen by Catanese et a].…”

Section: Discussionsupporting

confidence: 89%

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1-(2,4-Dichlorobenzyl)-1 H-lndazole-3-Carboxylic Acid (DICA), an Exfoliative Antispermatogenic Agent in the Rat

Lobl¹

1979

Archives of Andrology

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The oral administration of 50 mg DICNkg at nine weekly or four monthly intervals produced partially reversible infertility in male rats as judged by the results of serial mating and testicular histology. Oral 500 mg DICNkg doses administered at the same intervals produced permanent sterility. Single oral doses of 50 or 500 mg DICMkg elevated mean FSH concentrations on days 2, 3, and 7 but did not affect LH or testosterone. Mean plasma concentration peaked at 74 pghl 4 hr after a 50 mg/kg dose of uniformly tritiated DICA; 24 hr later, it had declined rapidly to 5.5 &ml. The drug did not have a strong affinity for any tissue studied including the testis. DICA-induced exfoliation of immature germ cells was first observed 4 hr after administration and led to significantly reduced testis weights by day 2. Neither single doses of 10-250 mg DICNkg nor five daily doses of 10-100 mg DICMkg reduced seminal vesicle, ventral prostate, or body weights of male rats. Chronic weekly DICA administration did reduce mean seminal vesicle weight. These studies have shown that DICA is an effective, partially reversible antifertility agent that directly affects the rat testis.

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Section: Discussionsupporting

confidence: 89%

“…The serum and testicular absorption profile was similar to that seen by Catanese et a]. [2] but peaked later. This was partially due to Ixge variations in absorption rate from rat to rat that skewed the mean values to longer times.…”

Section: Discussionsupporting

confidence: 83%

1-(2,4-Dichlorobenzyl)-1 H-lndazole-3-Carboxylic Acid (DICA), an Exfoliative Antispermatogenic Agent in the Rat

Lobl¹

1979

Archives of Andrology

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“…The method is simple, requiring only a liquid-liquid extraction step with ethyl acetate and sufficiently sensitive for monitoring the serum level of the drug administered at antispermatogenic doses in the rat (Catanese et al, 1978;Silvestrini et al, 1984) or at anticancer doses in man .…”

Section: Discussionmentioning

confidence: 99%

“…In the testis, the concentration of this drug, given at the same dose, reached a maximum after about 1 h, with a concentration of about 8 mg/g (Catanese et al, 1978). However, due to the low sensitivity of the method, the kinetics of the drug in plasma and testis were not followed for more than 24 and 8 h, respectively (Catanese et al, 1978). 2.…”

Section: Introductionmentioning

confidence: 99%

“…By fluorimetry, it was determined that the maximum plasma level of LND, administered to rats at the antispermatogenic dose of 112 mg/kg body weight (bw), was higher than 100 mg/mL after 30 min (Catanese et al, 1978). In the testis, the concentration of this drug, given at the same dose, reached a maximum after about 1 h, with a concentration of about 8 mg/g (Catanese et al, 1978). However, due to the low sensitivity of the method, the kinetics of the drug in plasma and testis were not followed for more than 24 and 8 h, respectively (Catanese et al, 1978).…”

Section: Introductionmentioning

confidence: 99%

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Analysis of lonidamine in rat serum and testis by high performance liquid chromatography

Grippa

Gatto

Leone

et al. 2001

Biomedical Chromatography

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A HPLC method for the determination of lonidamine in serum and testis, suitable for pharmacological studies in the rat and other mammals, has been developed. Briefly, 0.5 mL of serum or about 0.2 g of testicular tissue were extracted with ethyl acetate and evaporated to dryness under nitrogen. The residue was redissolved in methanol and an aliquot was injected onto a C18 column eluted with a mobile phase consisting of acetonitrile:water (51:49, v/v), containing 0.1% trifluoroacetic acid. The eluate was monitored at 230 nm with a sensitivity of 0.05 AUFS. By this method, the pharmacokinetics and the serum and testicular levels of the drug up to 120 h after the administration of one single dose (100 mg/kg body weight) of lonidamine to Sprague-Dawley rats have been studied. Results were highly variable, as previously reported, but a very good linear correlation was found between the serum and the testicular levels, suggesting that, in the rat, and possibly in the human, testicular levels could be estimated based on the serum concentrations.

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Enthalpy of formation for indazoles (indazole, 1H-indazole-3-carboxylic acid, 1H-indazole-5-carboxylic acid, 1H-indazole-6-carboxylic acid and 1-methyl-1H-indazole-6-carboxylic methyl ester): experimental and theoretical studies

Orozco-Guareño

Campos

Bárcena-Soto

et al. 2019

J Therm Anal Calorim

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A comparative study of serum and testicular concentrations of af 1312/TS (or 1-[(4-chlorophenyl)methyl] 1H-indazole-3-carboxylic acid) and diclondazolic acid (or 1-[(2,4-dichlorophenyl)methyl)]-1H-indazole-3-carboxylic acid) in rats

Cited by 9 publications

References 3 publications

1-(2,4-Dichlorobenzyl)-1 H-lndazole-3-Carboxylic Acid (DICA), an Exfoliative Antispermatogenic Agent in the Rat

1-(2,4-Dichlorobenzyl)-1 H-lndazole-3-Carboxylic Acid (DICA), an Exfoliative Antispermatogenic Agent in the Rat

Analysis of lonidamine in rat serum and testis by high performance liquid chromatography

Enthalpy of formation for indazoles (indazole, 1H-indazole-3-carboxylic acid, 1H-indazole-5-carboxylic acid, 1H-indazole-6-carboxylic acid and 1-methyl-1H-indazole-6-carboxylic methyl ester): experimental and theoretical studies

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