The selective 5-HT2 receptor antagonist amperozide attenuates 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane-induced inhibition of male rat sexual behavior

Klint, Thorsten; Dahlgren, I.Lena; Larsson, Knut

doi:10.1016/0014-2999(92)90336-3

Cited by 29 publications

(17 citation statements)

References 23 publications

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“…Thus, the male rat ejaculatory behaviour o ers a sensitive and reliable model to pharmacologically di erentiate 5-HT 1A from 5-HT 1B receptor agonists. The selectivity of the model receives support from the fact that 5-HT 2 receptor agonists, or antagonists, do not have speci®c e ects on male rat ejaculatory behaviour (Watson & Gorzalka, 1991;Klint et al, 1992;FernandezGuasti & Rodriguez-Manzo, 1992;Ahlenius & Larsson, 1998). However, the possible role of a number of recently cloned 5-HT receptor subtypes, such as 5-HT 4 , 5-HT 5 , 5-HT 6 and 5-HT 7 receptors (for example Lucas & Hen, 1995), in male rat ejaculatory behaviour must await the development of selective and speci®c pharmacological tools to study the functional importance of these newly identi®ed receptors.…”

Section: Discussionmentioning

confidence: 99%

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT_1Aand 5‐HT_1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Hillegaart

Ahlénius

1998

British J Pharmacology

117

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1 Ejaculatory problems and anorgasmia are well-known side-e ects of the SSRI antidepressants, and a pharmacologically induced increase in serotonergic neurotransmission inhibits ejaculatory behaviour in the rat. In the present study the role of 5-HT 1A and 5-HT 1B receptors in the mediation of male rat ejaculatory behaviour was examined by use of selective agonists and antagonists acting at these 5-HT receptor subtypes. 2 The 5-HT 1A receptor agonist 8-OH-DPAT (0.25 ± 4.00 mmol kg 71 s.c.) produced an expected facilitation of the male rat ejaculatory behaviour, and this e ect was fully antagonized by pretreatment with the new selective 5-HT 1A receptor antagonist (R)-3-N,N-dicyclobutylamino-8-¯uoro-3,4-dihydro-2H-1-benzopyran-5-carboxamide hydrogen (2R,3R) tartrate monohydrate (NAD-299) (1.0 mmol kg 71 s.c.). NAD-299 by itself (0.75 ± 3.00 mmol kg 71 s.c.) did not a ect the male rat ejaculatory behaviour. 3 The 5-HT 1B receptor agonist anpirtoline (0.25 ± 4.00 mmol kg 71 s.c.) produced a dose-dependent inhibition of the male rat ejaculatory behaviour, and this e ect was fully antagonized by pretreatment with the 5-HT 1B receptor antagonist isamoltane (16 mmol kg 71 s.c.) as well as by the new and selective antagonist (R)-(+)-2-(3-morpholinomethyl-2H-chromene-8-yl)oxymethylmorpholino methansulphonate (NAS-181) (16 mmol kg 71 s.c.). Isamoltane (1.0 ± 16.0 mmol kg 71 s.c.) and NAD-181 (1.0 ± 16.0 mmol kg 71 s.c.) had no, or weakly facilitatory e ects on the male rat ejaculatory behaviour. The non-selective 5-HT 1 receptor antagonist (7)-pindolol (8 mmol kg 71 s.c.), did not antagonize the inhibition produced by anpirtoline.4 The present results demonstrate opposite e ects, facilitation and inhibition, of male rat ejaculatory behaviour by stimulation of 5-HT 1A and 5-HT 1B receptors, respectively, suggesting that the SSRIinduced inhibition of male ejaculatory dysfunction is due to 5-HT 1B receptor stimulation.

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Section: Discussionmentioning

confidence: 99%

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT_1Aand 5‐HT_1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Hillegaart

Ahlénius

1998

British J Pharmacology

117

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“…50 On the other hand, several other studies have shown that 5-HT 2A/2C receptor agonists generally inhibit sexual behavior by decreasing the number of animals that initiated copulation, but do not affect ejaculation latencies in animals that do initiate copulation. [51][52][53] Thus, it appears that 5-HT 2 receptors in general inhibit sexual behavior, but their precise role in the regulation of ejaculation is not entirely clear.…”

Section: Serotonin Serotonergic Receptors and Ejaculatory Behaviormentioning

confidence: 99%

Psychopharmacology of male rat sexual behavior: modeling human sexual dysfunctions?

et al. 2006

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Most of our current understanding of the neurobiology, neuroanatomy and psychopharmacology of sexual behavior and ejaculatory function has been derived from preclinical studies in the rat. When a large population of male rats is tested on sexual activity during a number of successive tests, over time individual rats display a very stable sexual behavior that is either slow, normal or fast as characterized by the number of ejaculations performed. These sexual endophenotypes are postulated as rat counterparts of premature (fast rats) or retarded ejaculation (slow rats). Psychopharmacology in these endophenotypes helps to delineate the underlying mechanisms and pathology. This is illustrated by the effects of serotonergic antidepressants and serotonergic compounds on sexual and ejaculatory behavior of rats. These preclinical studies and models contribute to a better understanding of the neurobiology of ejaculation and boost the development of novel drug targets to treat ejaculatory disorders such as premature and retarded ejaculation.

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“…It has been shown that the 5-HT 2A/2C receptor agonist DOI suppresses sexual performance [18]and ejaculation [19]in rats, a blockade which is itself inhibited by pretreatment with the 5-HT 2 receptor antagonists LY 53 857 [18], ketanserin or mesulergine [19, 20]. No data on the involvement of discrete 5-HT 2 receptor subtypes on sexual arousal is available.…”

Section: Introductionmentioning

confidence: 99%

5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> Serotonin Receptors Differentially Modulate Mouse Sexual Arousal and the Hypothalamo-Pituitary-Testicular Response to the Presence of a Female

Попова¹,

Amstislavskaya²

2002

Neuroendocrinology

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The role of 5-HT_2A and 5-HT_2C subtypes of serotonergic receptors in the control of sexual behavior and plasma testosterone regulation was studied in male CBA mice exposed to a sexually receptive female separated by a transparent partition. Introduction of the receptive female induced sexual motivation and arousal in males, as evidenced by a prolonged time spent at the partition, unsuccessful attempts to step across it and a significant increase in plasma testosterone levels. Administration of 5-HT_2A receptor antagonists ketanserin (1.0 and 2.0 mg/kg i.p.) or cyproheptadine (1.0 and 2.0 mg/kg i.p.) diminished the behavioral components and prevented the hormonal components of male sexual arousal. Administration of the selective 5-HT_2C antagonist RS 102221 (1.0 and 2.0 mg/kg) considerably increased the time spent by males at the partition (p < 0.001) and, at the dose of 2.0 mg/kg, increased plasma testosterone levels (p < 0.01). Administration of ritanserin – a nonselective 5-HT_2A/2C antagonist and, to a smaller degree, 5-HT_2B antagonist – at doses of 0.1 and 0.5 mg/kg did not significantly influence male behavior and the activating effect of the presence of a female on the hypothalamo-pituitary-testicular system, although it increased resting testosterone levels (p < 0.05). The present findings suggest that 5-HT_2A/5-HT_2C receptors may be involved in the neural control of male sexual motivation and arousal, presumably by exerting reciprocal facilitative (5-HT_2A) or suppressive (5-HT_2C) influences.

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The selective 5-HT2 receptor antagonist amperozide attenuates 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane-induced inhibition of male rat sexual behavior

Cited by 29 publications

References 23 publications

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT_1Aand 5‐HT_1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT_1Aand 5‐HT_1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Psychopharmacology of male rat sexual behavior: modeling human sexual dysfunctions?

5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> Serotonin Receptors Differentially Modulate Mouse Sexual Arousal and the Hypothalamo-Pituitary-Testicular Response to the Presence of a Female

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The selective 5-HT2 receptor antagonist amperozide attenuates 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane-induced inhibition of male rat sexual behavior

Cited by 29 publications

References 23 publications

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT1Aand 5‐HT1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT1Aand 5‐HT1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Psychopharmacology of male rat sexual behavior: modeling human sexual dysfunctions?

5-HT<sub>2A</sub> and 5-HT<sub>2C</sub> Serotonin Receptors Differentially Modulate Mouse Sexual Arousal and the Hypothalamo-Pituitary-Testicular Response to the Presence of a Female

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Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT_1Aand 5‐HT_1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181

Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5‐HT_1Aand 5‐HT_1Breceptor agonists 8‐OH‐DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD‐299 and NAS‐181