Treatment of male sexual dysfunction

A technology for erectile dysfunction and men, which is specifically applied in the fields of MED, prevention and/or treatment of MSD, compound assays, and male erectile dysfunction. It can solve problems such as priapism, injection therapy is not as convenient as oral therapy, and achieves Effects of increasing penile blood flow and enhancing normal libido arousal response

Inactive Publication Date: 2004-05-12
PFIZER INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although injectable vasoactive drugs show high efficacy, side effects such as penile pain, fibrosis, and priapism are common, and injectable therapy is not as convenient as oral therapy, so sildenafil currently represents the most preferred drug on the market therapy

Method used

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  • Treatment of male sexual dysfunction
  • Treatment of male sexual dysfunction
  • Treatment of male sexual dysfunction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0814] Inhibition of the NPY Y1 receptor dose-dependently potentiates nerve-stimulated intracavernous pressure increases in an anesthetized rabbit model of erection

[0815] Submaximal increases in intracavernous pressure (ICP) induced by nerve stimulation were significantly increased (iv bolus) in the presence of increasing doses of a selective NPY Y1 receptor antagonist (BIBP3226). This increase became more pronounced at doses of 30 μg / kg and above. The greatest potentiation (approximately 127%) was observed at 30 [mu]g / kg. Data are expressed as percent increase (%), compared to the increase in control stimulation. Values ​​are expressed as mean ± s.e. mean. Unpaired comparison with control increase, *P<0.05, Student's t-test (see Figure 1).

[0816] NPY Y1 receptor antagonism had no apparent effect on basal / unstimulated intracavernous pressure.

Embodiment 2

[0818] PDE5 inhibition significantly increases the efficacy of PDE5 inhibitors to enhance penile erection in an anesthetized rabbit model

[0819] Intravenous administration (1 mg / kg) of a selective PDE5 inhibitor significantly enhanced the increase in ICP of nerve stimulation by 133±22% compared to the control increase. Data are presented as percent increase in ICP over control increase. Values ​​are expressed as mean ± s.e. mean. Unpaired comparison with control increase, *P<0.01, Student's t-test (see Figure 2).

[0820] PDE5 inhibition had no effect on basal / unstimulated intracavernous pressure.

Embodiment 3

[0822] Effects of drugs that increase intracavernous pressure on mean arterial blood pressure in anesthetized rabbits

[0823] In finding new treatments for male sexual dysfunction, such as MED, it is desirable that there be no associated cardiovascular side effects, such as effects on blood pressure or heart rate. In our study, we have found that the NPY Y1 receptor antagonist BIBP3226 (0.03-0.3mg / kg) has no substantial effect on blood pressure or heart rate, and this dose is similar to the increase in intracavernosus pressure induced by enhanced pelvic nerve stimulation.

[0824] Intravenous administration of BIBP3226 (a selective NPY Y1 antagonist) had no substantial effect on mean arterial blood pressure in an anesthetized rabbit model of penile erection. Figure 3 demonstrates that BIBP3226 has no significant effect on mean arterial pressure in anesthetized rabbits, and its dose-enhanced pelvic nerve stimulation increases cavernosal pressure. Mean arterial pressure (MAP) ...

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PUM

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Abstract

The use of an inhibitor of a neuropeptide Y (NPY), preferably of a NPY Y1 receptor, which inhibitor is selective for an NPY or NPY Y1 receptor associated with male genitalia, in the preparation/manufacture of a medicament for the treatment or prevention of male erectile dysfunction (MED).

Description

field of invention [0001] The present invention relates to compounds and medicaments useful for the treatment and / or prevention of male sexual dysfunction (MSD), in particular male erectile dysfunction (MED). [0002] The present invention also relates to methods of preventing and / or treating MSDs, in particular MEDs. [0003] The present invention also relates to assays for screening compounds useful in the treatment of MSDs, in particular MEDs. [0004] Abbreviations used hereinafter are listed before the claims section for convenience. Background of the invention [0005] Sexual dysfunction (SD) is a prominent clinical problem that affects both men and women. The cause of SD can be both organic and psychological. Organic SD is often caused by underlying vascular disease, such as those associated with hypertension or diabetes, and prescribed medication and / or psychiatric conditions, such as depression. Psychological factors include fear, behavioral anxiety, and interpe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/00A61K31/165G01N33/50A61K31/17A61K31/18A61K31/196A61K31/395A61K31/4015A61K31/433A61K31/4412A61K31/454A61K45/00A61K45/06A61P15/00A61P15/10G01N33/15G01N33/68
CPCA61K31/433A61K45/06A61K31/00A61K31/4015A61K31/17A61K31/454A61K31/395A61K31/18A61K31/165G01N33/689A61K31/4412G01N2500/00G01N2800/344A61K31/196A61P15/00A61P15/10A61K2300/00
Inventor A·M·内罗P·H·范德格拉夫C·P·维曼
Owner PFIZER INC
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