DL 111, a new non-hormonal antifertility agent: Contragestational and kinetic profile in baboons

Galliani, G.; Assandri, Alessandro; Lerner, Leonard J.; Omodei-Salè, A.; Lancini, Giancarlo; Nock, P.E.; Grant, Alison M.

doi:10.1016/0010-7824(82)90085-3

Cited by 16 publications

(2 citation statements)

References 15 publications

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“…1980. Madrid (Spain) The compound terminates pregnancy in all species so far investigated, namely, the mouse, the rat, the hamster, the rabbit, the dog (1,3) and the baboon (4). Its activity was shown to be dose, vehicle, route and time of pregnancy-dependent, with the most effective time for treatment being the early post-implantation period.…”

Section: Introductionmentioning

confidence: 99%

“…Data obtained with DL III-IT and an analogue (1, [3][4][5][6] demonstrated that, after parenteral administration, maximal effectiveness is obtained with multiple dose regimens and slow-release formulations, suggesting that a sustained availability of the active principle at the site of action (the utero-placental complex) is essential for pregnancy arrest. Therefore, in order to define the correlation between the anti-fertility and the kinetic profiles of DL III-IT, its activity and its disposition were studied in rats and hamsters after parenteral administration in different formulations.…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics-activity relationships of a new non-hormonal antifertility agent: 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1, 2,4-triazole, in the rat and the hamster

Assandri

Perazzi

Omodei-Salè

et al. 1983

European Journal of Drug Metabolism and Pharmacokinetics

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The pharmacokinetic profiles of a new non-hormonal anti-fertility agent, DL 111-IT, were studied in rats and hamsters given the 14C labelled compound parenterally dissolved in aqueous or oily vehicles. In both species, DL 111-It was rapidly metabolized and excreted when given intravenously or subcutaneously in aqueous vehicles (half-lives = 15-45 min.), whereas the kinetics were prolonged when it was administered in oily formulations (half-lives = 7-10 h). Binding studies revealed a high affinity of DL 111-IT for rat serum albumin (Ka = 6 X 10(5) 1/mole). The radioactivity concentrations in different tissues of pregnant rats appeared to be uniform with the excretory organs and lungs being the main target tissues. At the site of action, the utero-placental complex, the levels of total 14C were comparable to those in plasma, whereas the concentration of unchanged DL 111-IT was higher and remained so for a longer time. A comparison between the kinetic profiles and the activity data after single or multiple dose administration in different formulations, clearly indicates a close relationship between activity and plasma and tissue (utero-embryo placental complex) levels of DL 111-IT, and also makes clear the influence of the formulation and of the treatment schedule on the anti-fertility activity of the compound.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics-activity relationships of a new non-hormonal antifertility agent: 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1, 2,4-triazole, in the rat and the hamster

Assandri

Perazzi

Omodei-Salè

et al. 1983

European Journal of Drug Metabolism and Pharmacokinetics

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Design, Synthesis and Pregnancy‐Terminating Activity of 2‐Aryl Imidazo[2, 1 ‐a]isoquinolines

Shang

Tang

et al. 2004

Chin. J. Chem.

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In order to clarify the structural requirement of pregnancy-terminating drugs, the quantitative structure-activity relationship (QSAR) of 2-aryl imidazo[2,1-a]isoquhofines was studied on the basis of quantum mechanical calculation and multiple regression analysis. A Good correlation equation was obtained (?=0.925, q'=0.871). Some new compounds were designed according to the equation. Two of them, compounds 21 and 22, were synthesized and evaluated in NIH mice. The results showed that the difference of activity between 21 (median effective dose ED%=0.943 mgkglday) and 22 (ED%=1.099 mgkglday) was small and both of them were potent. It is also agreed with the computational results. Compared with L14105 which is the most potent pregnancy-terminating agent, these two compounds possess high activity. The evaluation of the anti-implanting activity showed that they were 100% effective at tested dosage 50.0,25.0, 12.5 mgkgldayX3 days in oral administration, which proved the both of them had anti-implanting activity and low first-pass effects.

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Non-steroidal menses-regulating agents: The present status

Mehrotra

Batra

Bhaduri

1995

Progress in Drug Research / Fortschritte Der Arzneimittelforschung / Progrès Des Recherches Pharmaceutiques

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DL 111, a new non-hormonal antifertility agent: Contragestational and kinetic profile in baboons

Cited by 16 publications

References 15 publications

Pharmacokinetics-activity relationships of a new non-hormonal antifertility agent: 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1, 2,4-triazole, in the rat and the hamster

Pharmacokinetics-activity relationships of a new non-hormonal antifertility agent: 3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1, 2,4-triazole, in the rat and the hamster

Design, Synthesis and Pregnancy‐Terminating Activity of 2‐Aryl Imidazo[2, 1 ‐a]isoquinolines

Non-steroidal menses-regulating agents: The present status

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