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Top PDE-5 Inhibitors and Where to Get them (Natural / Pharma)

top pde-5 pde-5 inhibitors icariin scrabrosolides xanthoparmelia horny goat weed top pde5i

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#1 Area-1255

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Posted 26 August 2014 - 08:36 PM


Think this is the right place for it, this should serve as helpful, especially for people looking for higher extracts of products.

 

TOP 5 PDE-5 Inhibitors and Where to Get Them

 

 

Stuff like Horny Goat Weed (high potency Icariin;natural PDE-5 inhibitor).

Xanthoparmelia Scabrosa is another potent one.

 

About and Research on Xanthoparmelia Scabrosa

 

Effect of Icariin on cyclic GMP levels and on the mRNA expression of cGMP-binding cGMP-specific phosphodiesterase (PDE5) in penile cavernosum.  (http://www.ncbi.nlm....pubmed/17120748)

 

 

To further investigate the mechanisms of action of icariin (ICA), we assessed the effects of ICA on the in vitro formation of cGMP and cAMP in isolated rabbit corpus cavernosum. Isolated segments of rabbit corpus cavernosum were exposed to increasing concentrations of ICA and the dose-dependent accumulation of cGMP and cAMP was determined in the tissues samples by means of 125I radioimmunoassay. Responses of the isolated tissues preparations to ICA were compared with those obtained with the reference compounds sildenafil (Sild). Furthermore, the effects of ICA on the mRNA expression of specific cGMP-binding phosphodiesterase type V (PDE5) in rat penis were also observed. After incubation with ICA for 6 h or 14 h respectively, the levels of PDE5 mRNA were examined by reverse transcriptase polymerase chain reaction (RT-PCR). The results showed that ICA increased cGMP concentrations directly (P < 0.05), but there was no significant effect on cAMP concentrations (P > 0.05). In the presence of sodium nitroprusside (SNP), a stimulatory agent of cGMP, both ICA and Sild increased cGMP concentrations with increasing dose (P < 0.01). Their EC50 was 4.62 (ICA) and 0.42 (Sild) micromol/L respectively. Under the same condition, ICA and Sild unaltered cAMP level significantly (P > 0.05). There were PDE5A1 and PDE5A2 mRNA expressions in rat corpus cavernosum with PDE5A2 being the dominant isoform. ICA could obviously inhibit these two isoforms mRNA expression in rat penis, and decrease PDE5A1 more pronouncedly (P < 0.01). The present study indicated that the aphrodisiac mechanisms of icariin involved the NO-cGMP signal transduction pathway, with increasing cGMP levels in the corpus cavernosum smooth muscle. The inhibitory effect of icariin on PDE5 mRNA expression, especially on PDE5A1, might account for its molecular mechanisms for its long-term activity.

 

 

 

 

 


Edited by Area-1255, 26 August 2014 - 08:37 PM.

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#2 Area-1255

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Posted 09 September 2014 - 12:28 AM

I haven't yet found a secondary Xantho study but if anyone can/has be helpful and chip in!


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#3 Area-1255

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Posted 30 September 2014 - 02:04 AM

Should add berberine and possibly gink to the list too.

 


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#4 Area-1255

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Posted 27 October 2014 - 10:28 PM

Updated with more references and compound info,.


Edited by Area-1255, 27 October 2014 - 10:28 PM.

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#5 Yunasa

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Posted 01 November 2014 - 06:25 PM

cool article! its good you know all this stuff, :) not many are able to dig all this up like that or don;t want to. :unsure:  :excl:  :ph34r:


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#6 Area-1255

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Posted 04 November 2014 - 08:48 PM

cool article! its good you know all this stuff, :) not many are able to dig all this up like that or don;t want to. :unsure:  :excl:  :ph34r:

People shouldn't have to perform all of the complex searches and inverse searches to find this - I aim to make more obscure information available in an easier to search manner - that way studies are collected and easy to access.


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#7 Area-1255

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Posted 26 November 2014 - 07:20 PM

Article updated on ICARIIN; added references on it's CALCIUM CHANNEL BLOCKING PROPERTIES!


Edited by Area-1255, 26 November 2014 - 07:21 PM.

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#8 Area-1255

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Posted 01 December 2014 - 05:40 PM

Any other ideas to add to this page / or any other natural PDE-5I's I haven't addressed?


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#9 Area-1255

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Posted 05 January 2015 - 06:14 PM

 

J Mol Graph Model. 2009 Oct;28(3):261-9. doi: 10.1016/j.jmgm.2009.08.004. Epub 2009 Aug 8.

Computational screening and design of traditional Chinese medicine (TCM) to block phosphodiesterase-5.
Abstract

The traditional Chinese medicines (TCM), Epimedium sagittatum (ESs), Cnidium monnieri (CMs), and Semen cuscutae (SCs), were used for treating erectile dysfunction since the ancient Han dynasty (202 BC-AD 220). Phosphodiesterase-5 (PDE-5) is deemed the target protein for inhibition to treat erectile dysfunction. In this study, a reliable multiple linear regression (MLR) model (r value=0.8484) was used to predict the activities of new candidates which were designed from ES, CM, and SC. From docking and pharmacophore analysis, the potent candidates among ES, CM, and SC were screened. SC01, SC03, and ES03b were predicted to have high potencies based on MLR analysis and high docking scores. Additionally, from our analysis, we make the follow conclusion (1) Hydrophobic compounds tend to be more potent PDE-5 inhibitors; (2) Because of the big binding site, inhibitors with molecular weights over 500 remain potent; (3) From the pharmacophore analysis, the features of hydrogen bond acceptors are the basis for designing novel inhibitors of PDE-5 and (4) According to MLR analysis, the number of ring groups could be up to 6, but the number of aromatic rings was limited to 4 to be potent. This study offers an alternative way to screen PDE-5 inhibitors from TCM and provides a scientific basis for confirming pharmacological actions of TCM.

PMID:   19747866   [PubMed - indexed for MEDLINE]

 


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#10 Area-1255

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Posted 22 January 2015 - 04:50 PM

http://www.ncbi.nlm....les/PMC2483323/

Pomegranate Juice: Is It the New, All-Natural Phosphodiesterase Type 5 Inhibitor?

 

 

Jacob Rajfer, MD

 

Pomegranate juice, which is derived from the pomegranate fruit, has been shown to have potent antioxidants, supposedly even more than in wine or green tea. It has recently been shown that it seems to protect nitric oxide (NO) in its continuing battle against oxidative stress, and it thereby has the potential to enhance the effect of NO on certain biologic systems.1 Because tumescence occurs as a result of an intact NO-cyclic guanosine monophosphate (cGMP) pathway within the cavernosal nerve and cavernosal smooth muscle cells, it seems logical to determine whether pomegranate juice can cause improvement in erectile function.

 


Edited by Area-1255, 22 January 2015 - 04:50 PM.

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#11 Area-1255

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Posted 05 February 2015 - 05:15 PM

http://www.raysaheli...diesterase.html

http://www.yourbrain...p?topic=14310.0


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#12 Area-1255

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Posted 26 February 2015 - 10:09 PM

UPDATE  : Added more information on Xanthoparmelia and the science behind it.


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#13 johnjuanb1

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Posted 02 March 2015 - 04:18 PM

I still find tadalafil to be my favorite PDE-5 inhibitor. I would like to give Avanafil a try. I use 25mg tadalifil for multiple purposes: vasodialation in skeletal muscles while lifting weights for maximal pump, reduces post workout lactic acid induced soreness, lowered blood pressure, and maximal erectile ability. I get tadalafil from SuperiorPeptide.com and get it 25% off with using the coupon code: JJ25

Tadalafil prevents acute heart failure with reduced ejection fraction in mice.

Authors
Salloum FN1, Chau VQ, Hoke NN, Kukreja RC.
Author information
Journal
Cardiovasc Drugs Ther. 2014 Dec;28(6):493-500. doi: 10.1007/s10557-014-6559-0.

Affiliation
Abstract
PURPOSE: Phosphodiesterase-5 (PDE5) inhibitors were shown to exert powerful protection in various animal models of cardiomyopathy. Tadalafil is a long-acting and highly specific PDE5 inhibitor, which makes it the most attractive in its class for long-term management of patients with heart failure. We studied the effects of tadalafil in attenuating ischemic cardiomyopathy in mice.

METHODS AND RESULTS: Adult male mice underwent myocardial infarction (MI) by permanent left coronary artery ligation and were treated daily with tadalafil (1 mg/kg; ip) or volume-matched 10% DMSO for 4 weeks. Twenty four hours after coronary ligation, infarct size, measured by TTC staining, was reduced from 70.1 ± 3.1% in DMSO-treated group to 49.3 ± 2.6% with tadalafil (P < 0.05). Similarly, tadalafil treatment yielded a smaller fibrotic area (8.8 ± 2.8% of LV), assessed by Masson's trichrome staining, as compared to DMSO group (21.9 ± 3.9%, P < 0.05). Apoptosis, measured by TUNEL assay, also declined with tadalafil (2.1 ± 0.2%) as compared to DMSO (6.7 ± 0.4%, P < 0.05) at 28 days post MI. Tadalafil also attenuated the increase in cardiac hypertrophy and pulmonary edema following infarction. These parameters reflect diminished left ventricular (LV) adverse remodeling and preserved fractional shortening with tadalafil at 7 and 28 days post infarction.

CONCLUSIONS: Tadalafil attenuates ischemic cardiomyopathy in mice and preserves LV function.
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#14 Area-1255

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Posted 02 March 2015 - 06:34 PM

I still find tadalafil to be my favorite PDE-5 inhibitor. I would like to give Avanafil a try. I use 25mg tadalifil for multiple purposes: vasodialation in skeletal muscles while lifting weights for maximal pump, reduces post workout lactic acid induced soreness, lowered blood pressure, and maximal erectile ability. I get tadalafil from SuperiorPeptide.com and get it 25% off with using the coupon code: JJ25

Tadalafil prevents acute heart failure with reduced ejection fraction in mice.

Authors
Salloum FN1, Chau VQ, Hoke NN, Kukreja RC.
Author information
Journal
Cardiovasc Drugs Ther. 2014 Dec;28(6):493-500. doi: 10.1007/s10557-014-6559-0.

Affiliation
Abstract
PURPOSE: Phosphodiesterase-5 (PDE5) inhibitors were shown to exert powerful protection in various animal models of cardiomyopathy. Tadalafil is a long-acting and highly specific PDE5 inhibitor, which makes it the most attractive in its class for long-term management of patients with heart failure. We studied the effects of tadalafil in attenuating ischemic cardiomyopathy in mice.

METHODS AND RESULTS: Adult male mice underwent myocardial infarction (MI) by permanent left coronary artery ligation and were treated daily with tadalafil (1 mg/kg; ip) or volume-matched 10% DMSO for 4 weeks. Twenty four hours after coronary ligation, infarct size, measured by TTC staining, was reduced from 70.1 ± 3.1% in DMSO-treated group to 49.3 ± 2.6% with tadalafil (P < 0.05). Similarly, tadalafil treatment yielded a smaller fibrotic area (8.8 ± 2.8% of LV), assessed by Masson's trichrome staining, as compared to DMSO group (21.9 ± 3.9%, P < 0.05). Apoptosis, measured by TUNEL assay, also declined with tadalafil (2.1 ± 0.2%) as compared to DMSO (6.7 ± 0.4%, P < 0.05) at 28 days post MI. Tadalafil also attenuated the increase in cardiac hypertrophy and pulmonary edema following infarction. These parameters reflect diminished left ventricular (LV) adverse remodeling and preserved fractional shortening with tadalafil at 7 and 28 days post infarction.

CONCLUSIONS: Tadalafil attenuates ischemic cardiomyopathy in mice and preserves LV function.

Thanks for the site reference and sound science!  :)


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#15 johnjuanb1

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Posted 02 March 2015 - 07:21 PM


I still find tadalafil to be my favorite PDE-5 inhibitor. I would like to give Avanafil a try. I use 25mg tadalifil for multiple purposes: vasodialation in skeletal muscles while lifting weights for maximal pump, reduces post workout lactic acid induced soreness, lowered blood pressure, and maximal erectile ability. I get tadalafil from SuperiorPeptide.com and get it 25% off with using the coupon code: JJ25

Tadalafil prevents acute heart failure with reduced ejection fraction in mice.

Authors
Salloum FN1, Chau VQ, Hoke NN, Kukreja RC.
Author information
Journal
Cardiovasc Drugs Ther. 2014 Dec;28(6):493-500. doi: 10.1007/s10557-014-6559-0.

Affiliation
Abstract
PURPOSE: Phosphodiesterase-5 (PDE5) inhibitors were shown to exert powerful protection in various animal models of cardiomyopathy. Tadalafil is a long-acting and highly specific PDE5 inhibitor, which makes it the most attractive in its class for long-term management of patients with heart failure. We studied the effects of tadalafil in attenuating ischemic cardiomyopathy in mice.

METHODS AND RESULTS: Adult male mice underwent myocardial infarction (MI) by permanent left coronary artery ligation and were treated daily with tadalafil (1 mg/kg; ip) or volume-matched 10% DMSO for 4 weeks. Twenty four hours after coronary ligation, infarct size, measured by TTC staining, was reduced from 70.1 ± 3.1% in DMSO-treated group to 49.3 ± 2.6% with tadalafil (P < 0.05). Similarly, tadalafil treatment yielded a smaller fibrotic area (8.8 ± 2.8% of LV), assessed by Masson's trichrome staining, as compared to DMSO group (21.9 ± 3.9%, P < 0.05). Apoptosis, measured by TUNEL assay, also declined with tadalafil (2.1 ± 0.2%) as compared to DMSO (6.7 ± 0.4%, P < 0.05) at 28 days post MI. Tadalafil also attenuated the increase in cardiac hypertrophy and pulmonary edema following infarction. These parameters reflect diminished left ventricular (LV) adverse remodeling and preserved fractional shortening with tadalafil at 7 and 28 days post infarction.

CONCLUSIONS: Tadalafil attenuates ischemic cardiomyopathy in mice and preserves LV function.

Thanks for the site reference and sound science! :)
You're welcome! :)
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#16 Area-1255

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Posted 22 March 2015 - 01:38 AM

Hopefully more PDE-5I's are available under the natural category - so we can find more viable stacks.


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#17 Area-1255

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Posted 12 April 2015 - 05:02 AM

If anybody has any suggestions be sure to LMK. http://www.med.miami.edu/


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#18 Yunasa

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Posted 14 April 2015 - 04:22 AM

If anybody has any suggestions be sure to LMK. http://www.med.miami.edu/

my uncle went to thatt school ! he is pHD


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#19 techguru75

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Posted 17 April 2015 - 02:38 AM

Has any one considered Red Kwao krua root extracts or as many call it butea superba root? Many Asian studies have shown results very impressive results compaired to big pharma PDE5 drugs. Eastern Medicine literature is hidden from us by the east but it doesn't help the FDA discrediting every translated one. What do you guys think of butea superba??
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#20 Area-1255

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Posted 17 April 2015 - 03:03 AM

Has any one considered Red Kwao krua root extracts or as many call it butea superba root? Many Asian studies have shown results very impressive results compaired to big pharma PDE5 drugs. Eastern Medicine literature is hidden from us by the east but it doesn't help the FDA discrediting every translated one. What do you guys think of butea superba??

Yes ; it's strong stuff. It mainly prevents the hydrolyzation/degradation of cAMP, though.

With that being said, it had some powerful anti-depressant effects, comparable to rolipram; very euphoric!!


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#21 Yunasa

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Posted 19 April 2015 - 03:12 AM

what i don't understand is why there arn't less of these studies being done on us gals ?


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#22 Area-1255

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Posted 19 April 2015 - 03:21 AM

what i don't understand is why there arn't less of these studies being done on us gals ?

There are. 

 

 

Psychiatr Serv. 1999 Aug;50(8):1076-8.

Sildenafil for women patients with antidepressant-induced sexual dysfunction.
Abstract

In an open study, sildenafil (Viagra) was prescribed for nine women outpatients who reported sexual dysfunction induced by antidepressant medication, primarily selective serotonin reuptake inhibitors. A 50 mg dose of sildenafil was prescribed, and patients were instructed to take it approximately one hour before sexual activity. They were told to increase the dose to 100 mg on the next occasion if they experienced a partial response or a lack of response to sildenafil. The nine patients, all of whom had experienced either anorgasmia or delayed orgasm with or without associated disturbances, reported significant reversal of sexual dysfunction, usually with the first dose of 50 mg of sildenafil.

PMID:   10445658   [PubMed - indexed for MEDLINE]

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#23 Area-1255

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Posted 20 April 2015 - 10:50 PM

Also there are even studies on AAS having benefits in women. 
Benefits and risks of testosterone treatment for hypoactive sexual desire disorder in women: a critical review of studies published in the decades preceding and succeeding the advent of phosphodiesterase type 5 inhibitor

 

JAMA. 1985 May 17;253(19):2871-3.

Anabolic steroid use and perceived effects in ten weight-trained women athletes.
Abstract

Ten women athletes who consistently used anabolic steroids were interviewed about their patterns of drug use and the perceived effects. Anabolic steroids were used in a cyclical manner, often with several drugs taken simultaneously. All participants believed that muscle size and strength were increased in association with anabolic steroid use. Most also noted a deepening of the voice, increased facial hair, increased aggressiveness, clitoral enlargement, and menstrual irregularities. The participants were willing to tolerate these side effects but thought that such changes might be unacceptable to many women.

PMID:   3989963   [PubMed - indexed for MEDLINE]

 


 

 


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#24 DeadBrain

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Posted 21 April 2015 - 10:33 PM

Hey  buddy! awesome post, i looove it. i love icariin and pde-5 inhib of all type and form ! thx for posten' this!



#25 Area-1255

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Posted 22 April 2015 - 12:16 AM

Hey  buddy! awesome post, i looove it. i love icariin and pde-5 inhib of all type and form ! thx for posten' this!

Thanks, "buddy"!


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#26 Junk Master

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Posted 22 April 2015 - 02:34 PM

Here's another vote for low dose Tadalafil taken on a daily basis.  No sides if taken low dose daily.  Increased pumps and recovery from workouts. 

 

I've never found any herbal supp that comes close.


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#27 Area-1255

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Posted 22 April 2015 - 07:08 PM

Here's another vote for low dose Tadalafil taken on a daily basis.  No sides if taken low dose daily.  Increased pumps and recovery from workouts. 

 

I've never found any herbal supp that comes close.

Thanks for the feedback, yes , if you have the means (or the $$$), every man should take a low-dose of Cialis to enhance PWO's or for pump. For average men with high test levels, only 2.5 mg - 5mg / day is all you need.  :)


Edited by Area-1255, 22 April 2015 - 07:09 PM.

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#28 nowayout

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Posted 22 April 2015 - 08:50 PM

Thanks for the feedback, yes , if you have the means (or the $$$), every man should take a low-dose of Cialis to enhance PWO's or for pump. For average men with high test levels, only 2.5 mg - 5mg / day is all you need.  :)

 

It is astronomically expensive, but nobody needs to pay those prices.  The Cipla generic tadalafil is sold for about a twentieth of the price of the brand name Cialis.  



#29 Area-1255

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Posted 22 April 2015 - 08:54 PM

 

Thanks for the feedback, yes , if you have the means (or the $$$), every man should take a low-dose of Cialis to enhance PWO's or for pump. For average men with high test levels, only 2.5 mg - 5mg / day is all you need.  :)

 

It is astronomically expensive, but nobody needs to pay those prices.  The Cipla generic tadalafil is sold for about a twentieth of the price of the brand name Cialis.  

 

Yeah but there's a lot of scams out there too, that's part of the issue...you know with the generic's and manufacturers from different countries. Re-sellers and what not, they can manipulate the goods and then offer it at a fraction of the original price.


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#30 magta39

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Posted 23 April 2015 - 12:50 AM

superiorpeptide.com claims to have liquid tadalafil drops, lostfalco has recommended this website


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