#1 Source for Hair Loss and Propecia: Hair Loss Starters Guide - Propecia - Avodart - Rogaine - Nizoral
Special Hairloss Topics: Hair Transplant Advice - Hair Replacement Advice - Female Hair Loss
Order Spectral DNC, Propecia and Avodart at hair2go.com
Ad: Propecia, Avodart, Spectral DNC and more!
Regrowth.com
Title: A possible explanation for the peripheral selectivity of a novel non-steroidal pure antiandrogen, Casodex (ICI 176,334).
Title Abreviation: Br J Cancer Date of Pub: 1989 Nov
Author: Freeman SN; Mainwaring WI; Furr BJ;
Issue/Part/Supplement: 5 Volume Issue: 60 Pagination: 664-8
MESH Headings: Androgen Antagonists (ME/*PD/PK); Anilides (ME/*PD/PK); Animal; Flutamide (PD); LH (BL); Male; Rats; Rats, Inbred Strains; Receptors, Androgen (ME); Support, Non-U.S. Gov't; Testosterone (BL); Tissue Distribution; -RN-;
Journal Title Code: AV4 Publication Type: JOURNAL ARTICLE
Date of Entry: 891215N Entry Month: 9002
Country: ENGLAND Index Priority: 1
Language: Eng Unique Identifier: 90028052
Unique Identifier: 90028052 ISSN: 0007-0920
Abstract: The in vivo antiandrogenicity of Casodex has been confirmed and characterised. Androgen receptor (AR) binding assays of rat ventral prostate gland cytosols revealed a relative binding affinity (RBA) for the AR of 0.267 and a k1 of 1.25 x 10(-7) M for Casodex. In addition, the peripheral selectivity of Casodex relative to other non-steroidal antiandrogens was confirmed in that daily treatment of non-castrated rats with Casodex (25 mg kg-1) did not elicit any changes in serum LH and testosterone concentrations relative to vehicle-treated controls, whereas elevated serum LH and testosterone were observed in rats treated with flutamide (25 mg kg-1). The peripheral selectivity of Casodex in the intact male rat was related to the distribution of radiolabelled antiandrogen following intravenous injection. All tissues with the exception of the hypothalamus and cerebral cortex (CC) sequestered radioactivity such that the tissue:serum ratio (TSR) for the drug was greater than unity. In the testis, the TSR was less than unity 1 h after injection but approached unity 5 h after injection and was greater than unity 10 h after injection. This may be explained by the presence of a blood-testis barrier for the drug, resulting in delayed equilibration between the blood and testis tissue. By comparison, an order of magnitude lower amounts of radioactivity in the hypothalamus and CC were maintained for the 10 h period after injection. These data, together with known physicochemical properties of Casodex suggest that a blood-brain barrier exists for the drug which results in exclusion of this antiandrogen from central sites of androgen negative feedback and that this accounts for its peripherally selective antihormonal profile.
Abstract By: Author
Address: Department of Biochemistry, University of Leeds, UK.
content2

Location:
Unknown

Location wrong? Click here
What's This?

Web
regrowth.com
Revivogen
Ad: Revivogen

More Info: Home | About Regrowth.com | How to Advertise | Privacy Policy | Advertising Policy | Contact Us
Site Map | Copyright © 2007 The Regrowth Network. All rights reserved. Legal Disclaimer

Other Cool Sites: Hair Loss Treatments - Body for Life Tracker - MedSpert

Propecia ® is a registered trademark of Merck. Avodart ® is a registered trademark of GlaxoSmithKline.
Rogaine ® is a registered trademark of Pfizer. Nizoral ® is a registered trademark of McNeil Consumer & Specialty Pharmaceuticals.