Ankit Agnihotri

Learn More
Centchroman, a non-steroidal antifertility agent showed a low affinity (Kd=13.19×10−6 M) and nonsaturable binding to human plasma. Centchroman did not complete either with sex hormone binding globulin or corticosteroid binding globulin. Polyacrylamide gel electrophoresis and temperature dependent binding characteristics revealed that the protein responsible(More)
Centchroman, a nonsteroidal antifertility agent was studied for its binding to monkey (Macaca mulatta) plasma proteins using charcoal adsorption and electrophoretic techniques. 14C-centchroman showed a low affinity binding and did not compete for 3H-cortisol or 3H-DHT binding sites in plasma. 14C-centchroman binding protein was heat stable in nature and(More)
The synthesis of C-nor-9,11-secoestradiol (4) has been achieved from 17 beta-acetoxy-11-chloro-3-methoxy-C-nor-9,11-secoestra-1,3,5(10)-tr ien-9-one (1) through a sequence of reactions without affecting the stereochemistry of estradiol-17 beta. Removal of the 9-keto function of 1 by hydrogenolysis and its subsequent treatment with Na/NH3 gives(More)
Progesterone-receptor binding affinity of some nonsteroidal molecules was assessed by competitive protein binding assay in rabbit as well as human uterine cytosol in vitro. Of 40 compounds belonging to 5 different series tested, 3-(p-anisoyl)-2-chloro-6, 7-dimethoxy-quinoline exhibited around 50% inhibition whereas 2-(p-anisoyl) naphthalene and(More)
A number of 2,6-dimethyl-3,5-bis(methoxycarbonyl)-4-substituted-1,4- dihydropyridines were synthesized and evaluated for pregnancy-interceptive activity in mated hamsters. Out of 24 compounds, 12, 15, 21, 22, 28, and 34 caused a marked reduction in the number of implantations when administered on days 3-8 postcoitum. In an in vitro competition assay, none(More)
Compound 84-182 prevented pregnancy when administered subcutaneously at 10 mg/kg dose on days 3-8 post-coitum in hamsters and on days 6-10 post-coitum in guinea pigs. At lower doses, while in hamsters there was a marked reduction in implantation number, majority of implantations in guinea pigs showed signs of resorption. The compound was ineffective when(More)
Levonorgestrel which binds with high affinity to SHBG, is suggested as a new radioligand for estimation of SHBG in human plasma. Using 3H-levonorgestrel as a ligand, a number of samples from men, women pregnant and non-pregnant were analysed. The SHBG content was lowest in men, low in women and rose to higher level during pregnancy. The results of the(More)
Some possible non-steroidal antiprogestins were evaluated for their receptor binding activity by competitive protein binding assay in rabbit as well as human uterine cytosol in vitro. Of the 42 compounds belonging to 5 different series tested, dimethyl ester of monobenzylidene succinic acid, 4-ethoxycarbonyl-3-(m-methoxybenzyl)-5-(m-anisyl)-gamma-butyrolact(More)
  • 1