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Screening Methods for the Evaluation of Antifertility Drugs

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Introduction to Basics of Pharmacology and Toxicology

Abstract

The discovery and development of a new antifertility drugs relies heavily on the preclinical use of animal models to establish efficacy and safety prior to trials in humans. Animal models have played a fundamental role in advancing our understanding of basic mechanisms and preclinical development of novel contraceptive drugs. Both in-vivo and in-vitro animal models are currently used for the screening of anti-fertility drugs. Presently, the in-vivo models are intended to screen the estrogenic, anti-estrogenic, progestational, anti-progestational, anti-ovulatory, anti-implantation activity, androgenic, anti-androgenic and anabolic activity in animals. These animals models which includes rats and mice used in in-vivo studies are either ovariectomized or immature. They should be maintained under controlled environmental conditions. Test preparations should be fresh, either in solution or in suspension in a suitable vehicle. In-vitro models are used to screen the assessment of sperm motility and count, its viability and morphology, estrogen and progesterone receptor binding activity, aromatase and 5-alpha reductase inhibition activity. Identification of drugs having anti-fertility activity is the need of current time and hence series of drug discoveries and development process is carried out. This chapter encompasses the comprehensive review of various animal models used for screening of various anti-fertility activities.

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Appendix

Appendix

1.1 Phases of Menstrual Cycle

An illustration depicts the ovarian cycle, body temperature, anterior pituitary hormones, ovarian hormones, and uterine cycle for ovulation from 0 to 28 days.

Image Source: Vios Fertility Institute.

1.2 Vaginal Opening Assay.

A set of 4 photographs depicts different phases of the vaginal opening in a mouse.

Appearance of the vagina in different phases of estrous cycle of an agouti strain mouse. a-Proestrus, b-Estrus, c- Metestrus, d- Diestrus.

[Reproduced From Byers SL, Wiles MV, Dunn SL, Taft RA (2012) Mouse Estrous Cycle Identification Tool and Images. PLoS ONE 7(4): e35538. https://doi.org/10.1371/journal.pone.0035538].

A set of 4 photographs depicts different phases of the vaginal opening in a white-coloured mouse.

1.3 Appearance of the vagina in different phases of estrous cycle of a Swiss albino strain mouse. a-Proestrus, b-Estrus, c- Metestrus, d- Diestrus

[Reproduced From Ekambaram G, Sampath Kumar SK, Joseph LD. Comparative Study on the Estimation of Estrous Cycle in Mice by Visual and Vaginal Lavage Method. J Clin Diagn Res. 2017 Jan;11(1):AC05-AC07. doi: 10.7860/JCDR/2017/23977.9148. Epub 2017 Jan 1. PMID: 28273958; PMCID: PMC5324403.]

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Gnanasegaran, S., Adhimoolam, M. (2022). Screening Methods for the Evaluation of Antifertility Drugs. In: Lakshmanan, M., Shewade, D.G., Raj, G.M. (eds) Introduction to Basics of Pharmacology and Toxicology. Springer, Singapore. https://doi.org/10.1007/978-981-19-5343-9_38

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  • DOI: https://doi.org/10.1007/978-981-19-5343-9_38

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