Mestranol
From DrugPedia: A Wikipedia for Drug discovery
(3 intermediate revisions not shown.) | |||
Line 1: | Line 1: | ||
+ | [http://172.141.127.22/raghava/hmrbase/test_extract.php?db=arun&table=nphormonet&id=1087&show=SHOW-3D Show 3-D Structure] | ||
+ | |||
'''Mestranol''' is the 3-[[methyl]] [[ether]] of [[ethinylestradiol]]. It was the [[estrogen]] used in many of the [[combined oral contraceptive pill|first oral contraceptives]]. | '''Mestranol''' is the 3-[[methyl]] [[ether]] of [[ethinylestradiol]]. It was the [[estrogen]] used in many of the [[combined oral contraceptive pill|first oral contraceptives]]. | ||
Line 11: | Line 13: | ||
'''Activity''' Estrogen | '''Activity''' Estrogen | ||
{| border="1;width:100%; height:200px;style=text-align:center" | {| border="1;width:100%; height:200px;style=text-align:center" | ||
- | |+'''Physiochemical properties of | + | |+'''Physiochemical properties of Mestranol:''' |
|- | |- | ||
! style="background:brown; color:white" |Physical Property | ! style="background:brown; color:white" |Physical Property |
Current revision
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
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 |
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. |