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Bilter
(@bilter)
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12/08/2020 10:26 am  

Ipamorelin, the first selective growth hormone secretagogue

K Raun, BS Hansen, NL Johansen, H Thogersen, K Madsen, M Ankersen, and PH Andersen
Department of GH Biology, Novo Nordisk A/S, Malov, Denmark.

The development and pharmacology of a new potent growth hormone (GH) secretagogue, ipamorelin, is described. Ipamorelin is a pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2), which displays high GH releasing potency and efficacy in vitro and in vivo. As an outcome of a major chemistry programme, ipamorelin was identified within a series of compounds lacking the central dipeptide Ala-Trp of growth hormone-releasing peptide (GHRP)-1. In vitro, ipamorelin released GH from primary rat pituitary cells with a potency and efficacy similar to GHRP-6 (ECs) = 1.3+/-0.4nmol/l and Emax = 85+/-5% vs 2.2+/-0.3nmol/l and 100%). A pharmacological profiling using GHRP and growth hormone-releasing hormone (GHRH) antagonists clearly demonstrated that ipamorelin, like GHRP-6, stimulates GH release via a GHRP-like receptor. In pentobarbital anaesthetised rats, ipamorelin released GH with a potency and efficacy comparable to GHRP-6 (ED50 = 80+/-42nmol/kg and Emax = 1545+/-250ng GH/ml vs 115+/-36nmol/kg and 1167+/-120ng GH/ml). In conscious swine, ipamorelin released GH with an ED50 = 2.3+/-0.03 nmol/kg and an Emax = 65+/-0.2 ng GH/ml plasma. Again, this was very similar to GHRP-6 (ED50 = 3.9+/-1.4 nmol/kg and Emax = 74+/-7ng GH/ml plasma). GHRP-2 displayed higher potency but lower efficacy (ED50 = 0.6 nmol/kg and Emax = 56+/-6 ng GH/ml plasma). The specificity for GH release was studied in swine. None of the GH secretagogues tested affected FSH, LH, PRL or TSH plasma levels. Administration of both GHRP-6 and GHRP-2 resulted in increased plasma levels of ACTH and cortisol. Very surprisingly, ipamorelin did not release ACTH or cortisol in levels significantly different from those observed following GHRH stimulation. This lack of effect on ACTH and cortisol plasma levels was evident even at doses more than 200-fold higher than the ED50 for GH release. In conclusion, ipamorelin is the first GHRP-receptor agonist with a selectivity for GH release similar to that displayed by GHRH. The specificity of ipamorelin makes this compound a very interesting candidate for future clinical development.


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Pieterv
(@pieterv)
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Joined: 1 year ago
Posts: 11
12/08/2020 3:11 pm  

I like it, it's a nice addition to GHRP-2/6
And it is especially recommended if you have trouble sleeping when using the mod GRF(1-29) and GHRP-2 or 6 combo (either as replacement for the GHRP, or as an addition with a lowered GHRP dose)


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motomatt
(@motomatt)
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Joined: 2 years ago
Posts: 53
12/08/2020 3:35 pm  

Re: Ipamorelin Thank you, for the information on Ipamorelin.

Posted by: Bilter
Ipamorelin, the first selective growth hormone secretagogue

K Raun, BS Hansen, NL Johansen, H Thogersen, K Madsen, M Ankersen, and PH Andersen
Department of GH Biology, Novo Nordisk A/S, Malov, Denmark.

The development and pharmacology of a new potent growth hormone (GH) secretagogue, ipamorelin, is described. Ipamorelin is a pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2), which displays high GH releasing potency and efficacy in vitro and in vivo. As an outcome of a major chemistry programme, ipamorelin was identified within a series of compounds lacking the central dipeptide Ala-Trp of growth hormone-releasing peptide (GHRP)-1. In vitro, ipamorelin released GH from primary rat pituitary cells with a potency and efficacy similar to GHRP-6 (ECs) = 1.3+/-0.4nmol/l and Emax = 85+/-5% vs 2.2+/-0.3nmol/l and 100%). A pharmacological profiling using GHRP and growth hormone-releasing hormone (GHRH) antagonists clearly demonstrated that ipamorelin, like GHRP-6, stimulates GH release via a GHRP-like receptor. In pentobarbital anaesthetised rats, ipamorelin released GH with a potency and efficacy comparable to GHRP-6 (ED50 = 80+/-42nmol/kg and Emax = 1545+/-250ng GH/ml vs 115+/-36nmol/kg and 1167+/-120ng GH/ml). In conscious swine, ipamorelin released GH with an ED50 = 2.3+/-0.03 nmol/kg and an Emax = 65+/-0.2 ng GH/ml plasma. Again, this was very similar to GHRP-6 (ED50 = 3.9+/-1.4 nmol/kg and Emax = 74+/-7ng GH/ml plasma). GHRP-2 displayed higher potency but lower efficacy (ED50 = 0.6 nmol/kg and Emax = 56+/-6 ng GH/ml plasma). The specificity for GH release was studied in swine. None of the GH secretagogues tested affected FSH, LH, PRL or TSH plasma levels. Administration of both GHRP-6 and GHRP-2 resulted in increased plasma levels of ACTH and cortisol. Very surprisingly, ipamorelin did not release ACTH or cortisol in levels significantly different from those observed following GHRH stimulation. This lack of effect on ACTH and cortisol plasma levels was evident even at doses more than 200-fold higher than the ED50 for GH release. In conclusion, ipamorelin is the first GHRP-receptor agonist with a selectivity for GH release similar to that displayed by GHRH. The specificity of ipamorelin makes this compound a very interesting candidate for future clinical development.

Don't buy upgrades, ride up grades.

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Bilter
(@bilter)
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12/08/2020 3:54 pm  

I started Ipamorelin / Mod GRF 1-29 @ 100mcg / 100mcg 8 days ago. I'll post up how it works in comparison to the GHRP 6 / CJC stack I typically have run in the past.


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rhinofight
(@rhinofight)
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12/08/2020 4:16 pm  

I use it in combo with Mod GRF and GHRP2 2-3 times per day.


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Seabiscuit Hogg
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12/08/2020 4:44 pm  
Posted by: Bilter
I started Ipamorelin / Mod GRF 1-29 @ 100mcg / 100mcg 8 days ago. I'll post up how it works in comparison to the GHRP 6 / CJC stack I typically have run in the past.

I'd be very interested in this since I'm running CJC/GHRP-6 now. I'm 8 days in also. It seems like it would be easier to manage carbs on the Mod GRF 1-29.

Seabiscuit Hogg is a fictious internet character. It is not recommended that you receive medical advice from fictious internet characters.

SBH :)


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Bilter
(@bilter)
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12/08/2020 5:04 pm  
Posted by: Seabiscuit Hogg
I'd be very interested in this since I'm running CJC/GHRP-6 now. I'm 8 days in also. It seems like it would be easier to manage carbs on the Mod GRF 1-29.

there is really no difference in management of carbs or fats. You get higher peak GH pulse with mod GRF 1-29 and lower troughs. I don't get the hunger with Ipamorelin that I got with GHRP-6. From what i have read though the GH peak is slightly less than with GRPP-6 or GHRP-2 for that matter. The lack of hunger is a nice thing, esepcially for my pre bed or pre morning cardio pin.

Given that I tend to not have issues with prolactin I may give GHRP-2 a try mid mod GRF my next run. It a bit cheaper and provides a higher GH peak......... but that is for another day


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freakinhuge
(@freakinhuge)
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12/08/2020 5:21 pm  

some very good peptide info, thanks


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Bilter
(@bilter)
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Joined: 2 years ago
Posts: 167
12/08/2020 5:46 pm  

Now on week 6 of my GRF / Ipam peptide cycle. I should also mention that I am also running Test-Enth'>test e/ Tren E@ 600mg / 400mg PW.
My goal at the start of this was to lose bf. My abdominal skinfold at day 1 was 11mm. Currently that is down to 7.5mm. BW is down approx 6 pounds so weight is coming off nicely, not too fast but I do seem to have stalled out in the last 10-14 days.

The best benefit I notice to date is reduction in everyday pain. I actually did not realize how much pain I was in day to day. When I began this I would place a hand on my knee to help myself up from a stooped position. I no longer do that. My back feels better, my knees feel MUCH better! Sleep in deeper and less broken. I have to also add that in my last peptide cycle which spanned approx. 12 months I think the quality of the peptides were very questionable. I now use clinical grade and the difference is huge.


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jboldman
(@jboldman)
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Posts: 1440
12/08/2020 6:06 pm  

that sounds like a great cycle.


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Tribe78
(@tribe78)
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Joined: 6 months ago
Posts: 3
12/08/2020 6:31 pm  

I just started Ipamorelin and GRF 1-29 at 100/100 mornings and before bed.

Ive gotta say - I have had the worst 3 nights sleep of my life! Terrible restless leg, and mind wont shut off!!!!! Maybe only a few hours of broken sleep a night. Im not sure I can do another night like that.

I keep hearing people's experiences with Ipamorelin is there are getting good rest!

Is anyone else having trouble sleeping like me?


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kataking
(@kataking)
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Posts: 27
12/08/2020 7:00 pm  
Posted by: trudy78
I just started Ipamorelin and GRF 1-29 at 100/100 mornings and before bed.

Ive gotta say - I have had the worst 3 nights sleep of my life! Terrible restless leg, and mind wont shut off!!!!! Maybe only a few hours of broken sleep a night. Im not sure I can do another night like that.

I keep hearing people's experiences with Ipamorelin is there are getting good rest!

Is anyone else having trouble sleeping like me?

cut the dose back to 50/50 for a few days or a week. maybe just do once a day for a while as well.
Once your body adjusts you should get really good sleep.

The restless leg thing my not be related, I have never experienced that from the peps. I have had that problem when dehydrated or electrolytes out of balance though.

Dr. Chrisler is giving a talk on Sermorelin at the A4M National convention in December so he isnt giving out a bunch of Information before then.


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Bilter
(@bilter)
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Joined: 2 years ago
Posts: 167
12/08/2020 7:16 pm  

Some results of my recent cycle..... week 9


Without befores these really do not tell the story. For reference when I started this my abdominal skin fold was 11mm, it is now down to 6mm. Things are going well and I feel very good..


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Seabiscuit Hogg
(@seabiscuit-hogg)
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12/08/2020 7:18 pm  

You're doing a really good job Bilter! How much cardio are you doing and how do you time it with pulse?

Seabiscuit Hogg is a fictious internet character. It is not recommended that you receive medical advice from fictious internet characters.

SBH :)


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Bilter
(@bilter)
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Joined: 2 years ago
Posts: 167
12/08/2020 7:40 pm  

Thanks, I am doing only 25 minutes of fasted am cardio 3 days per week. I'll take my peptides when I awaken, drink 2 cups of coffee and go


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