Competition of Phenothiazines with Oestradiol for Oestradiol Receptors in Rat Brain

Shani, J.; Givant, Y.; Sulman, F. G.; Eylath, Uri; Eckstein, B.

doi:10.1159/000122016

Cited by 23 publications

(4 citation statements)

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“…Our findings that a single administration of bromocrip tine increased specific 3H-Ei binding in the basal hypothal amus and anterior pituitary in the female rat extend the work of others in which bromocriptine administered for several days restored 3H-E2 binding in the pituitary after ei ther catecholamine depletion [8] or electrolytic lesion of the basal hypothalamus [12] in the female rat; the latter effect was believed to be independent of prolactin levels [12], The present findings are also consistent with observations that administration of perphenazine, which blocks DA recep tors, reduced uptake of 3H-E2 in the homogenate of hypo thalamus [58] and that administration of 6-hydroxydopamine to reduce endogenous catecholamines reduced 3H-E2 binding in the pineal and cerebellum and tended to reduce binding in the hypothalamus and pituitary [43]. The present report of a trend toward decreased binding of 3H-E2 in the homogenate of uterus after acute administration of bromo criptine may be consistent with reports that bromocriptine, both in vivo [13] and in vitro [17,40], reduced binding sites in the uterine cytosol incubated with 'H-Ei in vitro.…”

Section: Induction O F Sex Differences In 'H-ei Binding By Dopaminergsupporting

confidence: 92%

Sex Differences in [<sup>3</sup>H]-Estradiol Binding in Brain and Pituitary after Acute Dopaminergic Treatment

Gietzen¹,

Woolley²

1986

Neuroendocrinology

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Responses to estrogen differ between the sexes, yet sex differences in specific binding of estradiol (E2) to its receptor are not observed consistently. Dopaminergic treatment has been shown to increase binding of ³H-E₂ in selected brain areas and anterior pituitary in the female rat, and the dopaminergic system is sexually differentiated. In order to determine whether or not dopaminergic stimulation might induce sex differences in ³H-E₂ binding, male and female gonadectomized-adrenalectomized rats were pretreated either with bromocriptine, a dopamine agonist, or with diethyldithiocarbamate (DDC), an inhibitor of dopamine β-hydroxylase. DDC was used in order to increase endogenous release of dopamine. After such acute dopaminergic treatment, specific binding of ³H-E₂ in nuclear and extranuclear fractions of 6 brain areas and pituitary in vivo was determined 1 h after intravenous injection of Η-E₂ (1 µg/kg body weight). Administration of either bromocriptine or DDC increased specific ³H-E₂ binding to nuclear and extranuclear fractions of basal hypothalamus and anterior pituitary from female but not from male rats, thus inducing sex differences in binding in these two tissues. Bromocriptine also increased specific binding in the pineal in females. Total binding was increased in a crude membrane fraction (P₂) from pituitary of female but not of male rats after administration of DDC, but the percent of extranuclear specific binding found in the P₂ fraction was decreased after DDC in both males and females. The findings suggest that dopaminergic stimulation may induce sex differences in ³H-E2 binding by increasing binding in some brain areas and anterior pituitary in females but not in males.

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Section: Induction O F Sex Differences In 'H-ei Binding By Dopaminergsupporting

confidence: 92%

Sex Differences in [<sup>3</sup>H]-Estradiol Binding in Brain and Pituitary after Acute Dopaminergic Treatment

Gietzen¹,

Woolley²

1986

Neuroendocrinology

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“…We do not know which of the many well-documented pharmacological effects of CPZ underlie the changes seen in the present experiment. Influences of CPZ on the pituitary-gonadal and pituitary-adrenal systems (De Wied, 1967;Khazan, Mishkinsky, Ben-David, & Sulman, 1468;Shader & DiMascio, 1970;Shani (Mishkinsky), Gevant, Sulman, Eylath, & Eckstein, 1971) are particularly strong candidates in that manipulations of these systems during prenatal and early postnatal life have been shown to alter behavior (Ader, 1970;Beach, 1971;Bell, Drucker, &Woodruff, 1965;Grota and Ader, 1972;Lieberman, 1963;Swanson, 1966;Thompson, Goldenberg, Watson, & Watson, 1963;Ward, 1972). A simple alternative hypothesis is that the reduction of sensory and motor activity in the mother below an optimum level due to CPZ treatment may have generalized effects on fetal development.…”

Section: Discussionmentioning

confidence: 99%

Seizure susceptibility and avoidance conditioning in adult rats treated prenatally with chlorpromazine

Golub

Kornetsky

1974

Developmental Psychobiology

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Offspring of female rats treated early in gestation with clilorpromazine(CPZ) were tested at 30 days of age for seizure susceptibility and at 90 days of age for shock avoidance learning. Fostering procedures permitted separation of prenatal influences from postnatal rearing influences of drug treatment. Offspring of drug-treated mothers had higher avoidance scores, higher intertrial activity levels, and greater seizure susceptibility than offspring of controls. Animals reared by previously treated mothers also had higher avoidance and greater seizure susceptibility. This postnatal effect depended on sex and was not accompanied by an overall increase in intertrial activity. Rearing by a previously drug-treated mother was also found to modify the influence of neonatal stress on adult avoidance learning.Interest in the behavioral consequences of gestational treatment with psychoactive drugs has extended from observations of human newborns (Brazelton, 1970;Desmond, Rudolph, Hill, Claghorn, Dressen, & Burgdorff, 1969) to extensive behavioral testing of offspring of prenatally treated experimental animals (Joffe, 1969;Kornetsky, 1970;Werboff & Gottlieb, 1963;Young, 1967).Chlorpromazine (CPZ) is particularly interesting in this regard. It is not a teratogen (Beall, 1972) but has been shown to interfere with reproductive function at moderate doses in both humans (Beumont, Harris, Carr, Friesen, Kolakowska, MacKinnon, Mandelbrote, & Wiles, 1972; Shader & DiMascio, 1970) and animals (Murphree, Monroe, I% Seager, 1962; Ordy, Latanick, Johnson, & Massopust, 1963;Werboff & Dembicki, 1962) and to produce long-lasting biological changes in offspring (Ordy, Samorajski, Collins & Ralston, 1966;Tonge, 1973).In the present experiments, we consider the behavioral consequences in the adult rat of prenatal treatment with CPZ. In addition to adult behavior, we included measures of convulsive threshold as a general index of central nervous system excitability. We were also interested in determining whether prenatal treatment with CPZ would alter the influence of neonatal stress on later behavior.

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“…The presence of E receptors in the hypothalamus has been sufficiently demonstrated (39,40,41,42). The hypothalamus plays a decisive role in the regulation of BP and food intake.…”

Section: Discussionmentioning

confidence: 94%

The protective mechanism of estrogen on high blood pressure

Eiff

Lutz

Gries³

et al. 1985

Basic Res Cardiol

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In 2 series of experiments on 144 SHRSP, the influence of treatment with different doses of 17-beta-estradiolbenzoate (EB) (0.031, 0.125, 0.5 mg/kg EB or placebo) on the development of hypertension from the 9th to 22nd week of life (increase of blood pressure (BP) of untreated male rats from 178 to 252 mm Hg and of untreated female rats from 151 to 192 mm Hg) and in well established hypertension from the 23th to 36th weeks of life (male untreated rats 238 mm Hg (prior to the observation] was investigated. In both series, observation periods consisted of a therapy phase of 14 weeks and a follow-up phase of the same duration. The untreated female rats had a longer life-span (88.5 weeks) than the untreated male rats (68.0 weeks). The estrogen treatment of female animals had an effect on BP only with the highest dose of EB and had no effect on the life-span of the animals. However, in male rats, the development of hypertension was inhibited by EB. Male rats treated at an earlier stage had a life-span equal to that of the female animals. When hypertension was already well-established treatment with EB had an antihypertensive effect in male rats (BP fall: 27-36 mm Hg), but no prolongation of the life-span was obtained.

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Competition of Phenothiazines with Oestradiol for Oestradiol Receptors in Rat Brain

Cited by 23 publications

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Sex Differences in [<sup>3</sup>H]-Estradiol Binding in Brain and Pituitary after Acute Dopaminergic Treatment

Sex Differences in [<sup>3</sup>H]-Estradiol Binding in Brain and Pituitary after Acute Dopaminergic Treatment

Seizure susceptibility and avoidance conditioning in adult rats treated prenatally with chlorpromazine

The protective mechanism of estrogen on high blood pressure

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