Mestranol

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Mestranol is the 3-methyl ether of ethinylestradiol. It was the estrogen used in many of the first oral contraceptives.

It is a biologically inactive prodrug of ethinylestradiol to which it is demethylated in the liver with a conversion efficiency of 70% (50 µg of mestranol is pharmacokinetically bioequivalent to 35 µg of ethinylestradiol).<ref name=faigle>Template:Cite book</ref>

Pubchem(6291)

The 3-methyl ether of ETHINYL ESTRADIOL. It must be demethylated to be biologically active. It is used as the estrogen component of many combination ORAL CONTRACEPTIVES.

KEGG(C07618,D00575)

Activity Estrogen

Physiochemical properties of Mestranol:

Physical Property	Value	Units	Temp (deg C)	Source
Melting Point	150.5	deg C		EXP
log P (octanol-water)	4.680	(none)		EST
Atmospheric OH Rate Constant	9.04E-11	cm3/molecule-sec	25	EST

Toxicity:

Organism	Test Type	Route	Reported Dose (Normalized Dose)	Effect	Source
mouse	LD50	intraperitoneal	> 3200mg/kg (3200mg/kg)	SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) SKIN AND APPENDAGES (SKIN): HAIR: OTHER	Oyo Yakuri. Pharmacometrics. Vol. 4, Pg. 217, 1970.
mouse	LD50	oral	> 10gm/kg (10000mg/kg)	SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) SKIN AND APPENDAGES (SKIN): HAIR: OTHER	Oyo Yakuri. Pharmacometrics. Vol. 4, Pg. 217, 1970.
mouse	LD50	subcutaneous	2500mg/kg (2500mg/kg)	SENSE ORGANS AND SPECIAL SENSES: LACRIMATION: EYE SENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYE SKIN AND APPENDAGES (SKIN): HAIR: OTHER	Oyo Yakuri. Pharmacometrics. Vol. 4, Pg. 217, 1970.
rat	LD50	intraperitoneal	> 3gm/kg (3000mg/kg)	BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS SKIN AND APPENDAGES (SKIN): HAIR: OTHER	Oyo Yakuri. Pharmacometrics. Vol. 4, Pg. 217, 1970.
rat	LD50	oral	> 10gm/kg (10000mg/kg)		Oyo Yakuri. Pharmacometrics. Vol. 4, Pg. 217, 1970.
rat	LD50	subcutaneous	> 5gm/kg (5000mg/kg)	BEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY) GASTROINTESTINAL: CHANGES IN STRUCTURE OR FUNCTION OF SALIVARY GLANDS SKIN AND APPENDAGES (SKIN): HAIR: OTHER	Oyo Yakuri. Pharmacometrics. Vol. 4, Pg. 217, 1970.

References

Template:Sex hormonesde:Mestranol

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