5-HT1A receptor antagonists and lordosis behavior

Uphouse, Lynda; Andrade, Martha; Caldarola-Pastuszka, Marjay; Jackson, Astra

doi:10.1016/0028-3908(95)00196-4

Cited by 27 publications

(13 citation statements)

References 19 publications

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“…Direct application of 8-OH-DPAT into the VMH has been reported to suppress lordosis behavior and the effect was antagonized by injection with a 5-HT 1A antagonist, WAY-100135 (28). Direct injection with a toxin for serotonergic neurons into the VMH enhances lordosis (29).…”

Section: Discussionmentioning

confidence: 99%

Effects of 5-HT1A-Receptor Agonist, 8-OH-DPAT, and GABAB-Receptor Agonist, Baclofen, on Lordosis in Female Rats With Lesions in Either the Dorsal Raphe Nucleus or Septum

Kishitake

Yamanouchi

2005

J Pharmacol Sci

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Abstract. The inhibitory effects of 8-OH-DPAT, a 5-HT 1A -receptor agonist, and baclofen, a GABA B -receptor agonist, on lordosis were examined in estrogen and progesterone-treated ovariectomized rats with lesions in either the dorsal raphe nucleus (DRN) or septum and in rats with either sham lesions or no lesions. The first behavior test series was carried out 6 days after implantation of the rats with silicon tubes containing estradiol. Four hours after injection with 0.5 mg progesterone, behavioral tests were performed before and 30 min after an injection with 1 mg/ kg body weight 8-OH-DPAT. As a result, the mean lordosis quotient (LQ)s were changed from 100 to less than 20 before and after the injection in all groups. These results suggest that 8-OH-DPAT acts on areas other than the DRN and the septum, leading to a decrease in lordosis. Two weeks after implantation with estradiol, the next behavioral test series was carried out after injection with progesterone. Behavioral tests were performed before and after an injection with 10 mg baclofen. The results showed that the mean LQs decreased after the injection in all groups, but the mean LQ in the DRN lesion group was higher than that in the sham groups. These results indicate that baclofen may act partially on the DRN in inhibiting lordosis in female rats.

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Section: Discussionmentioning

confidence: 99%

Effects of 5-HT1A-Receptor Agonist, 8-OH-DPAT, and GABAB-Receptor Agonist, Baclofen, on Lordosis in Female Rats With Lesions in Either the Dorsal Raphe Nucleus or Septum

Kishitake

Yamanouchi

2005

J Pharmacol Sci

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“…Infusion of several 5-HT 1A receptor agonists [8-OH-DPAT, buspirone ([±)-l-(3-chlorophenyl)-2-[(l,l-dimethylethyl)amino]-l-propanone hydrochloride], 5-OH-DPAC [5-hydroxy-(3-di-n-propylamino)chroman] and 5-MEO-DPAC [5-methoxy-(3-di-n-propylamino)chroman] into this brain region rapidly inhibited lordosis behavior (Gonzalez et al, 1997; Uphouse et al, 1992b; Uphouse et al, 1993). When 8-OH-DPAT was used as the agonist, a variety of nonselective 5-HT 1A receptor antagonists, propanolol [(±)-1-isopropylamino-3-(1-naphthyloxy)-2-propanol hydrochloride] and pindolol [1-(1 H -indol-4-yloxy)-3-(isopropylamino)-2-propanol], as well as the selective 5-HT 1A receptor antagonist, WAY100635 [N-[2[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]N-(2 pyridinyl) cyclohexane-carboxamide trihydrochloride], prevented the effects of 8-OH-DPAT following infusion into the MBH (Uphouse et al, 1996a; Uphouse and Wolf, 2004). …”

Section: 0 Drugs Acting At 5-ht Receptorsmentioning

confidence: 99%

“…Moreover, most evidence indicates that 5-HT, by acting on 5-HT 1A receptors that exist in areas terminal to 5-HT neurons, are responsible for 5-HT 1A receptor agonists on lordosis behavior and that these receptors may not be tonically active in preventing the emergence of the behavior (Uphouse, 2000; Uphouse and Wolf, 2004). However, in rats with low sexual receptivity, both the neutral 5-HT 1A receptor antagonist, WAY100635, and the partial agonist/antagonist, WAY100135 [chiral N-t-butyl-3-(1-(4-(2-methoxy) phenyl)piperazinyl)-1-phenylpropionamide dihydrochloride, quarter hydrate], increased lordosis responding (Kishitake and Yamanouchi, 2004; Uphouse et al, 1996a). Moreover, when women with HSDD were treated with gepirone-extended release tablets, there was a significant reversal of HSDD in 63% of the patients (Fabre et al, 2011).…”

Section: 0 Drugs Acting At 5-ht Receptorsmentioning

confidence: 99%

“…Facilitation of the behavior in suboptimally hormonally-primed females was seen after treatment with either WAY100135 or SB 269970-A so it is currently impossible to exclude a role for 5-HT 7 receptors. However, evidence that the sexual behavioral effects of 8-OH-DPAT are blocked by both pindolol and WAY100635 (Uphouse et al, 1996a; Uphouse and Wolf, 2004), which have modest if any effect on 5-HT 7 receptors (Hannon and Hoyer, 2008; Lovenberg et al, 1993), enhances confidence in the conclusion that 5-HT 1A receptor agonists that have been studied reduce female sexual activity by interaction with 5-HT 1A receptors.…”

Section: 0 Drugs Acting At 5-ht Receptorsmentioning

confidence: 99%

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Pharmacology of serotonin and female sexual behavior

Uphouse

2014

Pharmacology Biochemistry and Behavior

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In this review, first a historical perspective of serotonin’s (5-HT) involvement in female sexual behavior is presented. Then an overview of studies implicating 5-HT is presented. The effect of drugs that increase or decrease CNS levels of 5-HT is reviewed. Evidence is presented that drugs which increase 5-HT have negative effects on female sexual behavior while a decrease in 5-HT is associated with facilitation of sexual behavior. Studies with compounds that act on 5-HT1, 5-HT2 or 5-HT3 receptors are discussed. Most evidence indicates that 5-HT1A receptor agonists inhibit sexual behavior while 5-HT2 or 5-HT3 receptors may exert a positive influence. There is substantial evidence to support a role for 5-HT in the modulation of female consummatory sexual behavior, but studies on the role of 5-HT in other elements of female sexual behavior (e.g. desire, motivation, sexual appetite) are few. Future studies should be directed at determining if these additional components of female sexual behavior are also modulated by 5-HT.

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“…A variety of drugs that increase extracellular 5-HT inhibit lordosis behavior but, depending on the receptor subtype activated, 5-HT receptor agonists can either inhibit or facilitate the behavior (Gonzalez et al, 1997; Hunter et al, 1985; Uphouse et al, 1996; Uphouse and Caldarola-Pastuszka, 1993; Wolf et al, 1998). The best characterized such agonists are the 5-HT 1A receptor agonists which rapidly inhibit lordosis behavior (Mendelson, 1992; Uphouse, 2000).…”

Section: 0 Introductionmentioning

confidence: 99%

Comparison of female Fischer and Sprague–Dawley rats in the response to ketanserin

Miryala

Hiegel

Uphouse

2013

Pharmacology Biochemistry and Behavior

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The effects of the 5-HT2A/2C receptor antagonist, ketanserin, on lordosis behavior were examined in hormonally primed, ovariectomized Fischer and Sprague-Dawley females. Rats were primed with 0.067 μg/g body weight estradiol benzoate and 3.33 μg/g body weight progesterone. After a pretest for sexual behavior, rats were injected with 0.416 to 10 mg/kg ketanserin. In both strains, lordosis behavior, lordosis quality, and proceptivity were significantly reduced by ketanserin. There was modest evidence of a strain difference with Sprague-Dawley females slightly more sensitive to ketanserin. In a second experiment, the effects of 10 mg/kg fluoxetine, 1 mg/kg ketanserin, and their combination were examined to determine if the two drugs would have additive effects on sexual behavior. There was no evidence that the drugs were additive in their effect and the strains did not differ in their response to the combined treatment. These findings are discussed in relation to prior evidence for strain differences in the sexual behavioral response to fluoxetine and to a receptor agonist acting preferentially at 5-HT1A receptors.

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5-HT1A receptor antagonists and lordosis behavior

Cited by 27 publications

References 19 publications

Effects of 5-HT1A-Receptor Agonist, 8-OH-DPAT, and GABAB-Receptor Agonist, Baclofen, on Lordosis in Female Rats With Lesions in Either the Dorsal Raphe Nucleus or Septum

Effects of 5-HT1A-Receptor Agonist, 8-OH-DPAT, and GABAB-Receptor Agonist, Baclofen, on Lordosis in Female Rats With Lesions in Either the Dorsal Raphe Nucleus or Septum

Pharmacology of serotonin and female sexual behavior

Comparison of female Fischer and Sprague–Dawley rats in the response to ketanserin

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