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All 24 posts Subject: Viagra Please login to post Thread doesn't expire Down

Gizmo23
(Stranger)
03-28-02 13:33
No 288975
      Viagra

I ´m just wondering, does anyone know what the molecule does look like or how to make it?

Rhodium
(Chief Bee)
03-28-02 13:47
No 288982
User Picture       Viagra/Sildenafil structure/synthesis
(Rated as: good read)

Here is a site describing the synthesis of Sildenafil, aka Viagra. A little too hard for the amateur to pull off.

http://www.ch.ic.ac.uk/local/projects/p_hazel/index.html

Greensnake
(Newbee)
03-28-02 17:28
No 289070
      not viagra

If interested in that therapeutic category, then go for vardenafil or cialis - simpler synthesis and better effects anyway.

Rhodium
(Chief Bee)
03-28-02 19:20
No 289115
User Picture       Vardenafil

Do you have any structure pics or a synthesis ref (patent?) - couldn't find anything but med-talk on google...

Gizmo23
(Stranger)
03-29-02 21:39
No 289576
      Vardenafil

THX guys smile

RoundBottom
(Hive Bee)
03-30-02 12:55
No 289837
      field report, biassay.

ok, i had mentioned earlier that i had recieved a small quantity of counterfeit/generic chinese viagra. due to my overwhelmingly porn star life style (it's not just a living, it's a well lubed living) i haven't had a chance to test it until today (like 3 months later).

appearance: #4 gel cap, packed with white powder, unmarked
dosage: unable to weigh, guessing close to 150mg
colour: plain white
consistancy: fine grainular powder (not fluffy)
taste: disagreeable, slightly bitter (not as bad as pure MDMA)

dosage taken: ~75mg, cap was opened, dumped and contents halved, one half take immediately

T+15: slight stomach nausea (tester has an empty stomach), slight gastrointestinal disturbance
T+30: minorly increased nausea
T+35: friend arrives, let the fun begin
T+35.17 wink : penis erect, and hard like it was really teased
T+40: intercourse
T+42: hard banging intercourse
T+44: neighbours laughing intercourse
T+46: lamp falls and blows bulb intercourse
T+47: how'd the couch get over here? intercourse
T+48: wow, i didn't know you could come so explosively climax
T+59: fluids replenished, respiratory rate calmed, playtime begins anew
T+61: eifel tower hard again (vive le chemistry!)
T+62: intercourse...
T+(that would be telling): ok, that's enough, we're too sore to continue

well, it's an unbridaled (pun intended) success. having not had any success with half of a 100mg real viagra (too low dosage probably), i must say this stuff is wonderful. nausea was persistant, and continued after effects of pill did. the other 75mg was ingested a couple hours (maybe T+320) later and more rooms were anihilated. erection could be 'disabled' for bathroom breaks, but the slightest stimulation caused arousal again.

i believe the wholesale cost on this stuff is about $0.75 a cap, or about $5 a gram. it is very popular to add viagra to MDMA for the gay community here, so this is a wholely suitable and cost effective method. with all the stuff they like in their E, i think we're looking at 00 caps now.

i can not hook anyone up or pass on any more information than this. all i'm trying to illustrate is that there are now chinese plants manufacturing generic viagra. we knew they would, just a matter of time.

enjoy, i know i will wink
i learned a thing or two from charlie dontcha know.

Greensnake
(Newbee)
03-30-02 17:32
No 289904
      vardenafil and cialis
(Rated as: excellent)

Unfortunately most info SWIM had is on now disassembled comp hard disc (nice pics and so)

Anyway, vardenafil patents:
Patent DE19750085
Patent DE19812462
Patent EP1049695
Patent WO9924433

Structural formula can be seen in this word doc
http://www.ama-assn.org/ama/upload/mm/365/vardenafil_dhcl.doc

Basically it's the same thing as sildenafil, but with one N atom shuffled to another place and Et instead of Me in tail. (haha... so much for Pfizers sildenafil patent protection) Synthesis is simpler than sildenafil's, but probably still too complicated for most.

Cialis patents:

Patent EP0740668
Patent JP1997508113
Patent US5859006
Patent US6025494
Patent US6127542
Patent WO9519978
Patent US6140329
Patent WO9703675
Patent US6143746

Cialis formula (again in Word document):

http://www.ama-assn.org/ama/upload/mm/365/tadalafil.doc

Now, cialis preparation is wholly within reach of persistent bee. Two biggest problems are starting material - D-tryptophan (unnatural isomer) and one chromatographic separation of diastereomers, which is needed. All other starting materials (piperonal, methylamine, chloroacetyl chloride) should be already more or less familiar to any well stocked bee.
---------
cool Make love, not war. cool

Precursor2112
(Hive Bee)
03-30-02 22:43
No 290011
User Picture       This is the reason

I logg on at the hive.

You could read the hive for a month to get one post like this.

What an eXcellent post on of the best I've ever read.

paranoid
03-31-02 06:28
      uhhh...
(Rated as: off-topic)

handsfull2
(Hive Bee)
03-31-02 07:50
No 290255
User Picture       uhhh

I second that.. but the post on chinese viagra was usefull .

Red my ass it was yellow when I saw it

RoundBottom
(Hive Bee)
03-31-02 08:58
No 290269
      you talking to me?

i'm baked? i don't know who you're refering to.

if you're wondering about the bioassay, the T+ stuff was a humourous diversion (a gentleman doesn't kiss and tell, and he always lies about a woman's age... remember that, younger bees). the rest of it should be considered serious content. oh, but the stomach nausea bit was true... and the lamp part wink .

i forgot to mention there was a slight rush, similar to a vitamin B/niacin(??) (the real vitamin B) rush/flush.
i learned a thing or two from charlie dontcha know.

pickler
(Greenhorn)
03-31-02 18:09
No 290425
User Picture       viagra

Take a 100mg viagra. They rock. Take a viagra and some mdma, it's incredible. Your dosage was probably too low, increase it and you'll have a better time. You had an upset stomach? First time swim heard that one. The only side effects swim has is a red face and a hard cock. tongue
We'll soon find out if I'm a chemist or not!

RoundBottom
(Hive Addict)
03-31-02 18:49
No 290435
      standard side effect.

> a red face and a hard cock.

which begat the other? wink

> You had an upset stomach?

yup, but it wasn't overly so. it's a standard side effect.

from the artice, above:

>Several side effects of sildenafil citrate were reported, during the
>trials as well as after marketing had started. The most commonly
>encountered are headaches, facial flushing, nasal congestion,
>urinary tract infection, diarrhea, upset stomach and muscle aches in
>the pelvic area.

i learned a thing or two from charlie dontcha know.

Rhodium
(Chief Bee)
10-05-03 16:23
No 462736
User Picture       The Discovery and Synthesis of Taladafil
(Rated as: excellent)

The Discovery of Tadalafil: A Novel and Highly Selective PDE5 Inhibitor. 1:
5,6,11,11a-Tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione Analogues
Alain Daugan, Pascal Grondin, Cécile Ruault, Anne-Charlotte Le Monnier de Gouville, Hervé Coste, Jorge Kirilovsky, François Hyafil, and Richard Labaudinière
J. Med. Chem., 46 (21), 4525-4532 (2003) (https://www.rhodium.ws/pdf/jmc-46-4525-2003-the-making-of-tadalafil-1.pdf)
DOI:10.1021/jm030056e

Abstract

Starting from ethyl -carboline-3-carboxylate (-CCE), 1, a modest inhibitor of type 5 phosphodiesterase (PDE5), a series of functionalized tetrahydro--carboline derivatives has been identified as a novel chemical class of potent and selective PDE5 inhibitors. Optimization of the side chain on the hydantoin ring of initial lead compound 2 and of the aromatic ring on position 5 led to the identification of compound 6e, a highly potent and selective PDE5 inhibitor, with greater selectivity for PDE5 vs PDE1-4 than sildenafil. Compound 6e demonstrated a long-lasting and significant blood pressure lowering effect after iv administration in the spontaneously hypertensive rat model but showed only moderate oral in vivo efficacy.

The Discovery of Tadalafil: A Novel and Highly Selective PDE5 Inhibitor. 2:
2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione Analogues
Alain Daugan, Pascal Grondin, Cécile Ruault, Anne-Charlotte Le Monnier de Gouville, Hervé Coste, Jean Michel Linget, Jorge Kirilovsky, François Hyafil, and Richard Labaudinière
J. Med. Chem., 46 (21), 4533 -4542 (2003) (https://www.rhodium.ws/pdf/jmc-46-4525-2003-the-making-of-tadalafil-2.pdf)
DOI:10.1021/jm0300577

Abstract

Modification of the hydantoin ring in the previously described lead compound 2a has led to the discovery of compound 12a, tadalafil, a highly potent and highly selective PDE5 inhibitor. The replacement of the hydantoin in compound 2a by a piperazinedione ring led to compound cis-11a which showed similar PDE5 inhibitory potency. Introduction of a 3,4-methylenedioxy substitution on the phenyl ring in position 6 led to a potent PDE5 inhibitor cis-11c with increased cellular potency. Optimization of the chain on the piperazinedione ring led to the identification of the racemic cis-N-methyl derivative 11i. High diastereospecificity for PDE5 inhibition was observed in the piperazinedione series with the cis-(6R,12aR) enantiomer displaying the highest PDE5 inhibitory activity. The piperazinedione 12a, tadalafil (GF196960), has been identified as a highly potent PDE5 inhibitor (IC₅₀ = 5 nM) with high selectivity for PDE5 vs PDE1-4 and PDE6. Compound 12a displays 85-fold greater selectivity vs PDE6 than sildenafil 1. 12a showed profound and long-lasting blood pressure lowering activity (30 mmHg/>7 h) in the spontaneously hypertensive rat model after oral administration (5 mg/kg).

RepVip
(Hive Bee)
10-11-03 04:29
No 463918
      A little off-topic.

A little off-topic.

http://www.nature.com/cgi-taf/DynaPage.taf?file=/nature/journal/v425/n6953/abs/nature01914_fs.html

Sorry I don't have access to the full article. However, this is an interesting article which gives the 3-dimensional shapes of viagara complexed with it's target (phosphodiesterase 5), as well as similar drugs used for erectile dysfunction.

It's interesting to know the 3-d shapes in that you can use them to "engineer" a more potent inhibitor, with hopefully less side-effects!

sushitake
(Newbee)
10-11-03 09:37
No 463951
      the blue lotus report

So in this link:Blue Lotus report 040502.p65 , is information by truman berst "master herbalist" on the phytochemistry of nymphaea caerulea.the author states that in a Vic Garners lab for forensic analysis the researchers put samples of the egyptian mummy "azru" through mass spectroscopy analysis. They found phytosterols,bioflavanoids, and the active ingredient of viagra,compounds known as phosphodiastrates. all of these compounds were assumed to be from the consumption of the nymphaea caerulea flowers. what I want to see is the actual phytochemical reports done on the flowers themselves. having taken the flowers before many times, in doses up to 10 grams, and definiteley feeling the effects, I would tend to believe this report. so whatcha think bees? is this for real?

opiophile

Lilienthal
(Moderator)
10-11-03 16:02
No 464007
User Picture       complete bullshit

That article (http://www.healthherbs.com/products/singleherbtinctures/3021.html) is complete bullshit from a sick (or stupid) brain. There is simpy nothing like "phosphodiastrates" and for sure it is not an ingredient of viagra. They just speculate that it might contain apomorphine. But from the wording you see that the author didn't understand a single word of what he wrote. He just wants to trick you into buying his dried herbs crazy . Read this for a real scientific work Medline (PMID=12493675).

thallium
(Hive Bee)
10-11-03 17:33
No 464023
      More about Nymphaea species here:

The sacred journey in dynastic Egypt: shamanistic trance in the context of the narcotic water lily and the mandrake.
Emboden W
J Psychoactive Drugs. 1989 Jan-Mar;21(1):61-75.
Medline (PMID=2656953)

The mushroom and the water lily: literary and pictorial evidence for Nymphaea as a ritual psychotogen in Mesoamerica.
Emboden WA.
J Ethnopharmacol. 1982 Mar;5(2):139-48.
Medline (PMID=7035751)

Transcultural use of narcotic water lilies in ancient Egyptian and Maya drug ritual.
Emboden WA.
J Ethnopharmacol. 1981 Jan;3(1):39-83.
Medline (PMID=7007741)

Video meliora proboque; Deteriora sequor. -Ovid

sushitake
(Newbee)
10-11-03 18:32
No 464036
      stupid bullshit
(Rated as: use [medline] or [doi] to link to articles!)

thanks for the links. I didnt find any phytochemical work in the "mummys curse" link however. There is a good report in: phytochemistry vol 51,issue 8 pages 1133-1137, that details flavanoids found in the flowers. I would still like to see a report that lists the occerance of Nuciferine in the flowers (I had seen a list of alkaloids in a book, forget the name, standard text, that described aporphine as BEING another name for nuciferine?)thanks again !!

opiophile

psyloxy
(Hive Addict)
10-16-03 16:51
No 465002
      blue lotus / sacred lily

Ordered 5g of a Nymphaea Caerulea 5:1 extract from a reliable ethnobotanicals dealer, had 2,5g each with 4cl 30% alcohol (said to increase effects) on two occasions - no effect whatsoever. It's a pity, the reports on erowid looked promising. May try the herb next time.

--psyloxy--

crocodile
(Stranger)
10-18-03 15:27
No 465418
      The effects are quite variable

I'm surprised you didn't feel ANYTHING but the effects are certainly very variable from person to person. For me personally Nymphaea caerulea (taken as decoction of 5-10g flowers) makes a pretty good sedative. It actually feels (physically) quite a bit like opiates but tends to be more sedating and much less euphoric. It is similar to Argemone mexicana but way stronger in my experience.

Some people actually DO report marked euphoria and other pleasant opiate-like symptoms... I plan to make a crude extract one day (one of those things which have been on my to-do list for a while now) to investigate this further... there is something quite appealing about this species.

Captain_America
02-09-04 03:11
      Go Pfizer Go, who cares about PiHKAL!?
(Rated as: insignificant)

morpheus
(Hive Addict)
02-12-04 00:33
No 487990
      Blue Lotus

Agree completely with Lilienthal.
The article has a couple oxymoron statements,
contradicts itself and is complete fiction.
Apomorphine is like syrup of ipecac in that
its made to make you puke your guts out.
How can you feel euphoric when after ralphing
all that is in your stomach you get the dry heaves
too.No there is no apomorphine in it anyways.Even if there was who would want it.It is used for poisonings in which the poison can come back up the same way it went down.In not all poisons is this beneficial.(Caustic for example)

Morf

Rhodium
(Chief Bee)
08-12-04 01:07
No 524929
User Picture       Eco-friendly Synthesis of Sildenafil (Viagra)
(Rated as: excellent)

The development of an environmentally benign synthesis of Sildenafil citrate (Viagra™)
Peter J. Dunn, Stephen Galvin and Kevin Hettenbach
Green Chemistry 6, 43–48 (2004) (https://www.rhodium.ws/pdf/viagra.eco-friendly.synthesis.pdf)

The process development and scale-up of the sildenafil citrate process is reviewed. Key environmental metrics are reported at several time points during the development process. Significant achievements during the development of sildenafil citrate were (i) discovering a convergent, efficient synthetic route (ii) designing 7 process steps so that there was no extractive work-up in any step (iii) implementing efficient solvent recovery early in the product’s commercial lifetime. The result of this work is that the E-factor for the process is very low with just 6 Kg of waste per kilogram of product compared with an industry average of 25–100 Kg. Pfizer received the 2003 UK Award for Green Chemical Technology (Best Process category) for the sildenafil citrate process.

^{The Hive - Clandestine Chemists Without Borders}

	https://the-hive.archive.erowid.org	the-hive@erowid.org



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	All 24 posts		Subject: Viagra		Please login to post		Thread doesn't expire		Down


		Gizmo23 (Stranger) 03-28-02 13:33 No 288975				Viagra
						I ´m just wondering, does anyone know what the molecule does look like or how to make it?



		Rhodium (Chief Bee) 03-28-02 13:47 No 288982				Viagra/Sildenafil structure/synthesis (Rated as: good read)
						Here is a site describing the synthesis of Sildenafil, aka Viagra. A little too hard for the amateur to pull off. http://www.ch.ic.ac.uk/local/projects/p_hazel/index.html



		Greensnake (Newbee) 03-28-02 17:28 No 289070				not viagra
						If interested in that therapeutic category, then go for vardenafil or cialis - simpler synthesis and better effects anyway.



		Rhodium (Chief Bee) 03-28-02 19:20 No 289115				Vardenafil
						Do you have any structure pics or a synthesis ref (patent?) - couldn't find anything but med-talk on google...



		Gizmo23 (Stranger) 03-29-02 21:39 No 289576				Vardenafil
						THX guys



		RoundBottom (Hive Bee) 03-30-02 12:55 No 289837				field report, biassay.
						ok, i had mentioned earlier that i had recieved a small quantity of counterfeit/generic chinese viagra. due to my overwhelmingly porn star life style (it's not just a living, it's a well lubed living) i haven't had a chance to test it until today (like 3 months later). appearance: #4 gel cap, packed with white powder, unmarked dosage: unable to weigh, guessing close to 150mg colour: plain white consistancy: fine grainular powder (not fluffy) taste: disagreeable, slightly bitter (not as bad as pure MDMA) dosage taken: ~75mg, cap was opened, dumped and contents halved, one half take immediately T+15: slight stomach nausea (tester has an empty stomach), slight gastrointestinal disturbance T+30: minorly increased nausea T+35: friend arrives, let the fun begin T+35.17: penis erect, and hard like it was really teased T+40: intercourse T+42: hard banging intercourse T+44: neighbours laughing intercourse T+46: lamp falls and blows bulb intercourse T+47: how'd the couch get over here? intercourse T+48: wow, i didn't know you could come so explosively climax T+59: fluids replenished, respiratory rate calmed, playtime begins anew T+61: eifel tower hard again (vive le chemistry!) T+62: intercourse... T+(that would be telling): ok, that's enough, we're too sore to continue well, it's an unbridaled (pun intended) success. having not had any success with half of a 100mg real viagra (too low dosage probably), i must say this stuff is wonderful. nausea was persistant, and continued after effects of pill did. the other 75mg was ingested a couple hours (maybe T+320) later and more rooms were anihilated. erection could be 'disabled' for bathroom breaks, but the slightest stimulation caused arousal again. i believe the wholesale cost on this stuff is about $0.75 a cap, or about $5 a gram. it is very popular to add viagra to MDMA for the gay community here, so this is a wholely suitable and cost effective method. with all the stuff they like in their E, i think we're looking at 00 caps now. i can not hook anyone up or pass on any more information than this. all i'm trying to illustrate is that there are now chinese plants manufacturing generic viagra. we knew they would, just a matter of time. enjoy, i know i will i learned a thing or two from charlie dontcha know.



		Greensnake (Newbee) 03-30-02 17:32 No 289904				vardenafil and cialis (Rated as: excellent)
						Unfortunately most info SWIM had is on now disassembled comp hard disc (nice pics and so) Anyway, vardenafil patents: Patent DE19750085 Patent DE19812462 Patent EP1049695 Patent WO9924433 Structural formula can be seen in this word doc http://www.ama-assn.org/ama/upload/mm/365/vardenafil_dhcl.doc Basically it's the same thing as sildenafil, but with one N atom shuffled to another place and Et instead of Me in tail. (haha... so much for Pfizers sildenafil patent protection) Synthesis is simpler than sildenafil's, but probably still too complicated for most. Cialis patents: Patent EP0740668 Patent JP1997508113 Patent US5859006 Patent US6025494 Patent US6127542 Patent WO9519978 Patent US6140329 Patent WO9703675 Patent US6143746 Cialis formula (again in Word document): http://www.ama-assn.org/ama/upload/mm/365/tadalafil.doc Now, cialis preparation is wholly within reach of persistent bee. Two biggest problems are starting material - D-tryptophan (unnatural isomer) and one chromatographic separation of diastereomers, which is needed. All other starting materials (piperonal, methylamine, chloroacetyl chloride) should be already more or less familiar to any well stocked bee. --------- Make love, not war.



		Precursor2112 (Hive Bee) 03-30-02 22:43 No 290011				This is the reason
						I logg on at the hive. You could read the hive for a month to get one post like this. What an eXcellent post on of the best I've ever read.



		paranoid 03-31-02 06:28				uhhh... (Rated as: off-topic)



		handsfull2 (Hive Bee) 03-31-02 07:50 No 290255				uhhh
						I second that.. but the post on chinese viagra was usefull . Red my ass it was yellow when I saw it



		RoundBottom (Hive Bee) 03-31-02 08:58 No 290269				you talking to me?
						i'm baked? i don't know who you're refering to. if you're wondering about the bioassay, the T+ stuff was a humourous diversion (a gentleman doesn't kiss and tell, and he always lies about a woman's age... remember that, younger bees). the rest of it should be considered serious content. oh, but the stomach nausea bit was true... and the lamp part . i forgot to mention there was a slight rush, similar to a vitamin B/niacin(??) (the real vitamin B) rush/flush. i learned a thing or two from charlie dontcha know.



		pickler (Greenhorn) 03-31-02 18:09 No 290425				viagra
						Take a 100mg viagra. They rock. Take a viagra and some mdma, it's incredible. Your dosage was probably too low, increase it and you'll have a better time. You had an upset stomach? First time swim heard that one. The only side effects swim has is a red face and a hard cock. We'll soon find out if I'm a chemist or not!



		RoundBottom (Hive Addict) 03-31-02 18:49 No 290435				standard side effect.
						> a red face and a hard cock. which begat the other? > You had an upset stomach? yup, but it wasn't overly so. it's a standard side effect. from the artice, above: >Several side effects of sildenafil citrate were reported, during the >trials as well as after marketing had started. The most commonly >encountered are headaches, facial flushing, nasal congestion, >urinary tract infection, diarrhea, upset stomach and muscle aches in >the pelvic area. i learned a thing or two from charlie dontcha know.



		Rhodium (Chief Bee) 10-05-03 16:23 No 462736				The Discovery and Synthesis of Taladafil (Rated as: excellent)
						The Discovery of Tadalafil: A Novel and Highly Selective PDE5 Inhibitor. 1: 5,6,11,11a-Tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione Analogues Alain Daugan, Pascal Grondin, Cécile Ruault, Anne-Charlotte Le Monnier de Gouville, Hervé Coste, Jorge Kirilovsky, François Hyafil, and Richard Labaudinière J. Med. Chem., 46 (21), 4525-4532 (2003) (https://www.rhodium.ws/pdf/jmc-46-4525-2003-the-making-of-tadalafil-1.pdf) DOI:10.1021/jm030056e Abstract Starting from ethyl -carboline-3-carboxylate (-CCE), 1, a modest inhibitor of type 5 phosphodiesterase (PDE5), a series of functionalized tetrahydro--carboline derivatives has been identified as a novel chemical class of potent and selective PDE5 inhibitors. Optimization of the side chain on the hydantoin ring of initial lead compound 2 and of the aromatic ring on position 5 led to the identification of compound 6e, a highly potent and selective PDE5 inhibitor, with greater selectivity for PDE5 vs PDE1-4 than sildenafil. Compound 6e demonstrated a long-lasting and significant blood pressure lowering effect after iv administration in the spontaneously hypertensive rat model but showed only moderate oral in vivo efficacy. The Discovery of Tadalafil: A Novel and Highly Selective PDE5 Inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione Analogues Alain Daugan, Pascal Grondin, Cécile Ruault, Anne-Charlotte Le Monnier de Gouville, Hervé Coste, Jean Michel Linget, Jorge Kirilovsky, François Hyafil, and Richard Labaudinière J. Med. Chem., 46 (21), 4533 -4542 (2003) (https://www.rhodium.ws/pdf/jmc-46-4525-2003-the-making-of-tadalafil-2.pdf) DOI:10.1021/jm0300577 Abstract Modification of the hydantoin ring in the previously described lead compound 2a has led to the discovery of compound 12a, tadalafil, a highly potent and highly selective PDE5 inhibitor. The replacement of the hydantoin in compound 2a by a piperazinedione ring led to compound cis-11a which showed similar PDE5 inhibitory potency. Introduction of a 3,4-methylenedioxy substitution on the phenyl ring in position 6 led to a potent PDE5 inhibitor cis-11c with increased cellular potency. Optimization of the chain on the piperazinedione ring led to the identification of the racemic cis-N-methyl derivative 11i. High diastereospecificity for PDE5 inhibition was observed in the piperazinedione series with the cis-(6R,12aR) enantiomer displaying the highest PDE5 inhibitory activity. The piperazinedione 12a, tadalafil (GF196960), has been identified as a highly potent PDE5 inhibitor (IC₅₀ = 5 nM) with high selectivity for PDE5 vs PDE1-4 and PDE6. Compound 12a displays 85-fold greater selectivity vs PDE6 than sildenafil 1. 12a showed profound and long-lasting blood pressure lowering activity (30 mmHg/>7 h) in the spontaneously hypertensive rat model after oral administration (5 mg/kg).



		RepVip (Hive Bee) 10-11-03 04:29 No 463918				A little off-topic.
						A little off-topic. http://www.nature.com/cgi-taf/DynaPage.taf?file=/nature/journal/v425/n6953/abs/nature01914_fs.html Sorry I don't have access to the full article. However, this is an interesting article which gives the 3-dimensional shapes of viagara complexed with it's target (phosphodiesterase 5), as well as similar drugs used for erectile dysfunction. It's interesting to know the 3-d shapes in that you can use them to "engineer" a more potent inhibitor, with hopefully less side-effects!



		sushitake (Newbee) 10-11-03 09:37 No 463951				the blue lotus report
						So in this link:Blue Lotus report 040502.p65 , is information by truman berst "master herbalist" on the phytochemistry of nymphaea caerulea.the author states that in a Vic Garners lab for forensic analysis the researchers put samples of the egyptian mummy "azru" through mass spectroscopy analysis. They found phytosterols,bioflavanoids, and the active ingredient of viagra,compounds known as phosphodiastrates. all of these compounds were assumed to be from the consumption of the nymphaea caerulea flowers. what I want to see is the actual phytochemical reports done on the flowers themselves. having taken the flowers before many times, in doses up to 10 grams, and definiteley feeling the effects, I would tend to believe this report. so whatcha think bees? is this for real? opiophile



		Lilienthal (Moderator) 10-11-03 16:02 No 464007				complete bullshit
						That article (http://www.healthherbs.com/products/singleherbtinctures/3021.html) is complete bullshit from a sick (or stupid) brain. There is simpy nothing like "phosphodiastrates" and for sure it is not an ingredient of viagra. They just speculate that it might contain apomorphine. But from the wording you see that the author didn't understand a single word of what he wrote. He just wants to trick you into buying his dried herbs . Read this for a real scientific work Medline (PMID=12493675).



		thallium (Hive Bee) 10-11-03 17:33 No 464023				More about Nymphaea species here:
						The sacred journey in dynastic Egypt: shamanistic trance in the context of the narcotic water lily and the mandrake. Emboden W J Psychoactive Drugs. 1989 Jan-Mar;21(1):61-75. Medline (PMID=2656953) The mushroom and the water lily: literary and pictorial evidence for Nymphaea as a ritual psychotogen in Mesoamerica. Emboden WA. J Ethnopharmacol. 1982 Mar;5(2):139-48. Medline (PMID=7035751) Transcultural use of narcotic water lilies in ancient Egyptian and Maya drug ritual. Emboden WA. J Ethnopharmacol. 1981 Jan;3(1):39-83. Medline (PMID=7007741) Video meliora proboque; Deteriora sequor. -Ovid



		sushitake (Newbee) 10-11-03 18:32 No 464036				stupid bullshit (Rated as: use [medline] or [doi] to link to articles!)
						thanks for the links. I didnt find any phytochemical work in the "mummys curse" link however. There is a good report in: phytochemistry vol 51,issue 8 pages 1133-1137, that details flavanoids found in the flowers. I would still like to see a report that lists the occerance of Nuciferine in the flowers (I had seen a list of alkaloids in a book, forget the name, standard text, that described aporphine as BEING another name for nuciferine?)thanks again !! opiophile



		psyloxy (Hive Addict) 10-16-03 16:51 No 465002				blue lotus / sacred lily
						Ordered 5g of a Nymphaea Caerulea 5:1 extract from a reliable ethnobotanicals dealer, had 2,5g each with 4cl 30% alcohol (said to increase effects) on two occasions - no effect whatsoever. It's a pity, the reports on erowid looked promising. May try the herb next time. --psyloxy--



		crocodile (Stranger) 10-18-03 15:27 No 465418				The effects are quite variable
						I'm surprised you didn't feel ANYTHING but the effects are certainly very variable from person to person. For me personally Nymphaea caerulea (taken as decoction of 5-10g flowers) makes a pretty good sedative. It actually feels (physically) quite a bit like opiates but tends to be more sedating and much less euphoric. It is similar to Argemone mexicana but way stronger in my experience. Some people actually DO report marked euphoria and other pleasant opiate-like symptoms... I plan to make a crude extract one day (one of those things which have been on my to-do list for a while now) to investigate this further... there is something quite appealing about this species.



		Captain_America 02-09-04 03:11				Go Pfizer Go, who cares about PiHKAL!? (Rated as: insignificant)



		morpheus (Hive Addict) 02-12-04 00:33 No 487990				Blue Lotus
						Agree completely with Lilienthal. The article has a couple oxymoron statements, contradicts itself and is complete fiction. Apomorphine is like syrup of ipecac in that its made to make you puke your guts out. How can you feel euphoric when after ralphing all that is in your stomach you get the dry heaves too.No there is no apomorphine in it anyways.Even if there was who would want it.It is used for poisonings in which the poison can come back up the same way it went down.In not all poisons is this beneficial.(Caustic for example) Morf



		Rhodium (Chief Bee) 08-12-04 01:07 No 524929				Eco-friendly Synthesis of Sildenafil (Viagra) (Rated as: excellent)
						The development of an environmentally benign synthesis of Sildenafil citrate (Viagra™) Peter J. Dunn, Stephen Galvin and Kevin Hettenbach Green Chemistry 6, 43–48 (2004) (https://www.rhodium.ws/pdf/viagra.eco-friendly.synthesis.pdf) The process development and scale-up of the sildenafil citrate process is reviewed. Key environmental metrics are reported at several time points during the development process. Significant achievements during the development of sildenafil citrate were (i) discovering a convergent, efficient synthetic route (ii) designing 7 process steps so that there was no extractive work-up in any step (iii) implementing efficient solvent recovery early in the product’s commercial lifetime. The result of this work is that the E-factor for the process is very low with just 6 Kg of waste per kilogram of product compared with an industry average of 25–100 Kg. Pfizer received the 2003 UK Award for Green Chemical Technology (Best Process category) for the sildenafil citrate process. ^{The Hive - Clandestine Chemists Without Borders}

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