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We have developed a redox-chemical system for brain-enhanced drug delivery of estradiol based on an interconvertible dihydropyridine in equilibrium with pyridinium salt carrier. Estradiol, when combined with the carrier, readily crosses the blood-brain barrier and upon oxidation of the carrier is "locked" in the brain. The aim of this study was to evaluate the effects of an estradiol-chemical delivery system (E2-CDS) versus an equimolar dose of estradiol-17-valerate (E2-VAL) on copulatory behavior in orchidectomized rats. The data revealed that a single dose of E2-CDS was more efficacious than E2-VAL in stimulating mounting behavior (percent responding) and the effect was 100% through 5 weeks. E2-CDS increased intromission behavior more than E2-VAL through 28 days. Mount and intromission latencies were reduced by E2-CDS to a greater extent and for a longer time (28 days) than E2-VAL. Neither form of estradiol restored ejaculation parameters or penile reflexes. These data suggest that E2-CDS causes a potent and long-acting stimulation of proceptive and consummatory components of male sexual behavior, presumably acting through the local brain-release of estradiol.
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
May 1990,
Drug design and delivery,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
January 1973,
Acta physiologica Scandinavica. Supplementum,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
August 1979,
Hormones and behavior,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
May 2001,
Hormones and behavior,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
October 1979,
Physiology & behavior,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
March 1984,
Hormones and behavior,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
December 1988,
Hormones and behavior,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
January 1973,
Acta physiologica Scandinavica. Supplementum,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
March 1979,
Activitas nervosa superior,
W R Anderson, and
J W Simpkins, and
M E Brewster, and
N Bodor
June 1974,
British journal of pharmacology,
