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Adverse Drug Reaction Reporting    FDA Warnings    Published Withdrawal Studies    Pregnancy Warnings    Forum Psychology

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Old 04-09-2012, 06:44 AM   #1
mike_yuk
 
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WAY-101405/100635 reverses and prevents sexual dysfunction

5-HT(1A) receptor antagonism reverses and prevents fluoxetine-induced sexual dysfunction in rats.
Int J Neuropsychopharmacol. 2009 Sep;12(:1045-53. Epub 2009 May 13.
Sukoff Rizzo SJ, Pulicicchio C, Malberg JE, Andree TH, Stack GP, Hughes ZA, Schechter LE, Rosenzweig-Lipson S.
Discovery Neuroscience, Wyeth Research, CN-8000, Princeton, NJ 08543, USA. rizzos@wyeth.com
Abstract:
Sexual dysfunction associated with antidepressant treatment continues to be a major compliance issue for antidepressant therapies. 5-HT(1A) antagonists have been suggested as beneficial adjunctive treatment in respect of antidepressant efficacy; however, the effects of 5-HT(1A) antagonism on antidepressant-induced side-effects has not been fully examined. The present study was conducted to evaluate the ability of acute or chronic treatment with 5-HT(1A) antagonists to alter chronic fluoxetine-induced impairments in sexual function. Chronic 14-d treatment with fluoxetine resulted in a marked reduction in the number of non-contact penile erections in sexually experienced male rats, relative to vehicle-treated controls. Acute administration of the 5-HT(1A) antagonist WAY-101405 resulted in a complete reversal of chronic fluoxetine-induced deficits on non-contact penile erections at doses that did not significantly alter baselines. Chronic co-administration of the 5-HT(1A) antagonists WAY-100635 or WAY-101405 with fluoxetine prevented fluoxetine-induced deficits in non-contact penile erections in sexually experienced male rats. Moreover, withdrawal of WAY-100635 from co-treatment with chonic fluoxetine, resulted in a time-dependent reinstatement of chronic fluoxetine-induced deficits in non-contact penile erections. Additionally, chronic administration of SSA-426, a molecule with dual activity as both a SSRI and 5-HT(1A) antagonist, did not produce deficits in non-contact penile erections at doses demonstrated to have antidepressant-like activity in the olfactory bulbectomy model. Taken together, these data suggest that 5-HT(1A) antagonist treatment may have utility for the management of SSRI-induced sexual dysfunction.








http://www.ncbi.nlm.nih.gov/pubmed/19435548
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Old 04-09-2012, 09:10 AM   #2
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Re: WAY-101405/100635 reverses and prevents sexual dysfunction

5-HT(1A) antagonists:
Alprenolol
AV-965
BMY-7,378
Cyanopindolol
Dotarizine
Flopropione
GR-46,611
Iodocyanopindolol
Isamoltane
Lecozotan
Methiothepin
Methysergide
MPPF
NAN-190
Oxprenolol
Pindobind
Pindolol
Propranolol
Quetiapine
Robalzotan
SB-649,915
SDZ-216,525
Spiperone
Spiramide
Spiroxatrine
UH-301
WAY-100,135
WAY-100,635
Xylamidine
source:
http://en.wikipedia.org/wiki/5-HT1A_receptor

Last edited by mike_yuk : 04-09-2012 at 09:12 AM. Reason: updating information
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Old 04-09-2012, 09:23 AM   #3
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Re: WAY-101405/100635 reverses and prevents sexual dysfunction

Doxazosin, ketanserin, and 5-HT(1A) and 5-HT(4) receptor antagonists may be useful as part of combination therapy used to treat erectile dysfunction.

http://www.andrologyjournal.org/cgi/.../full/27/5/679
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Old 04-09-2012, 12:28 PM   #4
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Re: WAY-101405/100635 reverses and prevents sexual dysfunction

A quick google shows that ketanserin is rarely used on humans, beyond that there's just no information on it. Doxazosin is Cardura, which will bottom out a normal blood pressure VERY fast. This "research" is from 2006 in the one link, and the other shows testing on rats only. The lack of follow up reporting pretty much tells the tale of effectiveness.
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Old 04-15-2012, 04:58 AM   #5
mike_yuk
 
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Re: WAY-101405/100635 reverses and prevents sexual dysfunction

I am going to try: Pindolol for premature ejaculation
It is 5-HT1A receptor antagonist, it may help me with erection as well, will see.
Some research, over Pindodol and premature ejaculation:
Article: http://www.ncbi.nlm.nih.gov/pubmed/18204339
about Pindol: http://en.wikipedia.org/wiki/Pindolol
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Old 04-15-2012, 12:41 PM   #6
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Re: WAY-101405/100635 reverses and prevents sexual dysfunction

Quote:
Originally Posted by mike_yuk View Post
I am going to try: Pindolol for premature ejaculation
It is 5-HT1A receptor antagonist, it may help me with erection as well, will see.
Some research, over Pindodol and premature ejaculation:
Article: http://www.ncbi.nlm.nih.gov/pubmed/18204339
about Pindol: http://en.wikipedia.org/wiki/Pindolol
Really....did you read the study?

"48 and 41 seconds to approximately 188 and 58 seconds". We're talking SECONDS delayed here and the risks of beta blockers to achieve those seconds. "The incidence of side effects with paroxetine-pindolol was significantly higher (P = 0.04)." The study makes no reference to erection quality.

Beta blockers significantly lower heart rate and blood pressure, this is a HUGE risk for someone with normal blood pressure.
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