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.