Effect of serotonin antagonists on prolactin and progesterone secretion in rats: evidence that the stimulatory and inhibitory actions of serotonin on prolactin release may be mediated through different receptors. 1988

G A Jahn, and R P Deis
Laboratorio de Reproduccion y Lactancia, CRICYT-CONICET, Mendoza, Argentina.

The serotoninergic regulation of prolactin release was studied in female rats in different reproductive states using ketanserin, a specific S2 receptor blocker, ICS 205-930 ((3 alpha-tropanyl)1H-indol-3-carboxylic acid ester), a specific S3 receptor blocker and p-chlorophenylalanine (pCPA), a serotonin synthesis inhibitor. Administration of ketanserin to pro-oestrous rats inhibited the afternoon prolactin surge; this inhibition was prevented by progesterone. On day 3 of pregnancy, pCPA or ketanserin blocked the afternoon prolactin surge, and administration of oestrogen (on day 2) and progesterone (on day 3) in combination, but not alone, prevented this effect. On day 9 of pregnancy, treatment with oestrogen (on day 8) and progesterone (on day 9) induced an afternoon surge of prolactin which was prevented by administration of ketanserin or pCPA. On days 9 and 16, pCPA induced a slight increase in serum prolactin in rats not treated with steroids, but ketanserin had no effect. On day 13, ketanserin and pCPA had no effect on serum prolactin levels, but after increasing serotoninergic transmission by injecting fluoxetine and 5-hydroxytryptophan, serum prolactin levels were decreased. On day 19, ketanserin produced a transient increase in the serum concentration of prolactin, probably produced by the marked decrease in the serum concentration of progesterone induced by the S2 receptor blocker. Administration of ICS 205-930 to pro-oestrous rats or rats on day 19 of pregnancy had no effect on serum concentrations of prolactin and progesterone.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D007650 Ketanserin A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients. 3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione,R-41,468,R-41468,R 41,468,R 41468,R41,468,R41468
D010134 Fenclonine A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin. p-Chlorophenylalanine,para-Chlorophenylalanine,CP-10,188,DL-3-(4-Chlorophenyl)alanine,Fenclonin,Fenclonine (L)-Isomer,Fenclonine Hydrobromide,Fenclonine Hydrochloride,Fenclonine, (D)-Isomer,Hydrobromide, Fenclonine,Hydrochloride, Fenclonine,para Chlorophenylalanine
D011247 Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. Gestation,Pregnancies
D011359 Proestrus A phase of the ESTROUS CYCLE that precedes ESTRUS. During proestrus, the Graafian follicles undergo maturation.
D011374 Progesterone The major progestational steroid that is secreted primarily by the CORPUS LUTEUM and the PLACENTA. Progesterone acts on the UTERUS, the MAMMARY GLANDS and the BRAIN. It is required in EMBRYO IMPLANTATION; PREGNANCY maintenance, and the development of mammary tissue for MILK production. Progesterone, converted from PREGNENOLONE, also serves as an intermediate in the biosynthesis of GONADAL STEROID HORMONES and adrenal CORTICOSTEROIDS. Pregnenedione,Progesterone, (13 alpha,17 alpha)-(+-)-Isomer,Progesterone, (17 alpha)-Isomer,Progesterone, (9 beta,10 alpha)-Isomer
D011388 Prolactin A lactogenic hormone secreted by the adenohypophysis (PITUITARY GLAND, ANTERIOR). It is a polypeptide of approximately 23 kD. Besides its major action on lactation, in some species prolactin exerts effects on reproduction, maternal behavior, fat metabolism, immunomodulation and osmoregulation. Prolactin receptors are present in the mammary gland, hypothalamus, liver, ovary, testis, and prostate. Lactogenic Hormone, Pituitary,Mammotropic Hormone, Pituitary,Mammotropin,PRL (Prolactin),Hormone, Pituitary Lactogenic,Hormone, Pituitary Mammotropic,Pituitary Lactogenic Hormone,Pituitary Mammotropic Hormone
D011985 Receptors, Serotonin Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action. 5-HT Receptor,5-HT Receptors,5-Hydroxytryptamine Receptor,5-Hydroxytryptamine Receptors,Receptors, Tryptamine,Serotonin Receptor,Serotonin Receptors,Tryptamine Receptor,Tryptamine Receptors,Receptors, 5-HT,Receptors, 5-Hydroxytryptamine,5 HT Receptor,5 HT Receptors,5 Hydroxytryptamine Receptor,5 Hydroxytryptamine Receptors,Receptor, 5-HT,Receptor, 5-Hydroxytryptamine,Receptor, Serotonin,Receptor, Tryptamine,Receptors, 5 HT,Receptors, 5 Hydroxytryptamine
D005260 Female Females
D005473 Fluoxetine The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants. Fluoxetin,Fluoxetine Hydrochloride,Lilly-110140,N-Methyl-gamma-(4-(trifluoromethyl)phenoxy)benzenepropanamine,Prozac,Sarafem,Lilly 110140,Lilly110140

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