Literature DB >> 2278844

Radioimmunoassay of 7 alpha-methyl-19-nortestosterone and investigation of its pharmacokinetics in animals.

N Kumar1, A K Didolkar, A Ladd, R Thau, C Monder, C W Bardin, K Sundaram.   

Abstract

A method for the measurement of 7 alpha-methyl-19-nortestosterone (7MENT) in serum/plasma by radioimmunoassay (RIA) is described. The antiserum, raised against 7 alpha-methyl-19-nortestosterone-3-O-oxime-bovine serum albumin, had a low titer (final dilution = 1:4500) and low affinity (Ka = 1.17 x 10(9) l/mol) but showed little or no cross-reactivity with several of the steroids tested. The sensitivity of the RIA was 28.2 pg/ml and the mean recovery of added cold steroid was 86 to 100%. Intra- and inter-assay coefficients of variation ranged from 4.3 to 7.3% and 7.3 to 8.4%, respectively. This RIA was used to follow plasma 7MENT levels after a single i.v. injection of the steroid in rats and rabbits. The metabolic clearance rates (MCR) of 7MENT as determined from the plasma disappearance curve for rats and rabbits were 50 l/day and 336 l/day, respectively. The MCR of 7MENT in rats and rabbits lies in the same range as for testosterone. When compared to other nortestosterone derivatives such as norethisterone, 7MENT is metabolized relatively faster.

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Year:  1990        PMID: 2278844     DOI: 10.1016/0960-0760(90)90405-a

Source DB:  PubMed          Journal:  J Steroid Biochem Mol Biol        ISSN: 0960-0760            Impact factor:   4.292


  7 in total

1.  The potent synthetic androgens, dimethandrolone (7α,11β-dimethyl-19-nortestosterone) and 11β-methyl-19-nortestosterone, do not require 5α-reduction to exert their maximal androgenic effects.

Authors:  Barbara J Attardi; Sheri A Hild; Sailaja Koduri; Trung Pham; Laurent Pessaint; Jean Engbring; Bruce Till; David Gropp; Anne Semon; Jerry R Reel
Journal:  J Steroid Biochem Mol Biol       Date:  2010-06-25       Impact factor: 4.292

2.  MIV-150-containing intravaginal rings protect macaque vaginal explants against SHIV-RT infection.

Authors:  Louise A Ouattara; Patrick Barnable; Paul Mawson; Samantha Seidor; Thomas M Zydowsky; Larisa Kizima; Aixa Rodriguez; José A Fernández-Romero; Michael L Cooney; Kevin D Roberts; Agegnehu Gettie; James Blanchard; Melissa Robbiani; Natalia Teleshova
Journal:  Antimicrob Agents Chemother       Date:  2014-03-10       Impact factor: 5.191

3.  The nonnucleoside reverse transcriptase inhibitor MIV-150 in carrageenan gel prevents rectal transmission of simian/human immunodeficiency virus infection in macaques.

Authors:  R Singer; N Derby; A Rodriguez; L Kizima; J Kenney; M Aravantinou; A Chudolij; A Gettie; J Blanchard; J D Lifson; M Piatak; J A Fernández-Romero; T M Zydowsky; M Robbiani
Journal:  J Virol       Date:  2011-03-16       Impact factor: 5.103

4.  7α-methyl-19-nortestosterone vs. testosterone implants for hypogonadal osteoporosis: a preclinical study in the aged male orchidectomized rat model.

Authors:  M Sinnesael; F Callewaert; M Morreels; N Kumar; R Sitruk-Ware; K Van Proeyen; P Hespel; S Boonen; F Claessens; D Vanderschueren
Journal:  Int J Androl       Date:  2011-07-26

5.  An intravaginal ring that releases the NNRTI MIV-150 reduces SHIV transmission in macaques.

Authors:  Rachel Singer; Paul Mawson; Nina Derby; Aixa Rodriguez; Larisa Kizima; Radhika Menon; Daniel Goldman; Jessica Kenney; Meropi Aravantinou; Samantha Seidor; Agegnehu Gettie; James Blanchard; Michael Piatak; Jeffrey D Lifson; José A Fernández-Romero; Melissa Robbiani; Thomas M Zydowsky
Journal:  Sci Transl Med       Date:  2012-09-05       Impact factor: 17.956

6.  An antiretroviral/zinc combination gel provides 24 hours of complete protection against vaginal SHIV infection in macaques.

Authors:  Jessica Kenney; Meropi Aravantinou; Rachel Singer; Mayla Hsu; Aixa Rodriguez; Larisa Kizima; Ciby J Abraham; Radhika Menon; Samantha Seidor; Anne Chudolij; Agegnehu Gettie; James Blanchard; Jeffrey D Lifson; Michael Piatak; Jose A Fernández-Romero; Thomas M Zydowsky; Melissa Robbiani
Journal:  PLoS One       Date:  2011-01-05       Impact factor: 3.240

7.  Exposure to MIV-150 from a high-dose intravaginal ring results in limited emergence of drug resistance mutations in SHIV-RT infected rhesus macaques.

Authors:  Mayla Hsu; Brandon F Keele; Meropi Aravantinou; Noa Krawczyk; Samantha Seidor; Ciby J Abraham; Shimin Zhang; Aixa Rodriguez; Larisa Kizima; Nina Derby; Ninochka Jean-Pierre; Olga Mizenina; Agegnehu Gettie; Brooke Grasperge; James Blanchard; Michael J Piatak; Jeffrey D Lifson; José A Fernández-Romero; Thomas M Zydowsky; Melissa Robbiani
Journal:  PLoS One       Date:  2014-02-27       Impact factor: 3.240

  7 in total

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