GABA-B Agonist Reverses Negative Feedback Effect of Testosterone on GnRH and LH Secretion in Male Sheep

(Of importance here is the fact that Phenibut is a derivative of Balcofen; the two are extremely simmilar).

[Size=4]A {gamma}-Aminobutyric AcidB Agonist Reverses the Negative Feedback Effect of Testosterone on Gonadotropin-Releasing Hormone and Luteinizing Hormone Secretion in the Male Sheep[/size]
[Size=4]Gary L. Jackson, Susanne G. Wood and David E. Kuehl
Department of Veterinary Biosciences, University of Illinois, Urbana, Illinois 61802[/size]
endo.endojournals.org/cgi/conten … 41/11/3940

Infusion of baclofen, a GABAB agonist, into the medial basal hypothalamus (MBH) of castrated rams rapidly increases LH pulse amplitude without altering pulse frequency. The objectives of this study were to determine whether baclofen infusion increased LH in testosterone (T)-treated and intact rams, the increased LH was due to increased GnRH release, and FSH secretion also was increased. In the first experiment we tested the main effects and interaction of baclofen and T on FSH and LH pulse patterns in castrated rams (n = 7). In the second experiment we determined whether baclofen affected GnRH and LH pulses in intact males. Microdialysis guide cannulae were implanted bilaterally into the MBH. After recovery of the animal from surgery, the MBH was perfused using concentric microdialysis probes (2-mm tip) with artificial cerebrospinal fluid (aCSF) for a 3-h control period followed by either aCSF or 1 mM baclofen for 4 h. Blood samples were taken at 10-min intervals. T suppressed mean LH concentrations (10.4 ± 1.3 vs. 3.3 ± 1.3 ng/ml) such that LH pulses were undetectable in some T-treated animals during the control period. The change (control period vs. drug infusion period) in mean LH was greater in response to baclofen than in response to aCSF and was not altered by T. The baclofen x T interaction was nonsignificant. Mean FSH was decreased by T, but was not altered by baclofen. In the second experiment hypophyseal portal blood was collected coincident with microdialysis. Infusion of baclofen into the MBH of intact males (n = 7) resulted within 1 h in the onset of frequent and robust GnRH pulses (0.10/h before baclofen vs. 1.57/h after baclofen) that were followed either immediately or gradually by coincident LH pulses. One interpretation is that baclofen acts downstream of the site of action of T. GABAB receptors may regulate pulse amplitude in both the presence and absence of T and regulate pulse frequency by modulating the inhibitory effect of T.

Agonists
GABA
Baclofen is a GABA analogue which acts as a selective agonist of GABAB receptors, and is used as a muscle relaxant. However, it can aggravate absence seizures, and so is not used in epilepsy.
gamma-Hydroxybutyrate
Phenibut
3-Aminopropylphosphinic acid
CGP-35024: 3-Aminopropyl(methyl)phosphinic acid, CAS# 127729-35-5, 10x more potent than baclofen as GABAB agonist, but also GABAC antagonist
CGP-44532

CGP-7930
[edit]Positive Allosteric Modulators
CGP-7930[9][10]
BHFF
BHF-177[11]
BSPP
GS-39783[12]

Source : en.wikipedia.org/wiki/GABAB_receptor

There was that one guy who recovered VIA GHB so you might be on to something. We’ve focused mainly on GABAA receptors given allopregnanlone and it’s action on making them more active.

I actually have some phenibut but apparently tolerance is built quickly and there is potential for some level of addiction.

Related:

forum.bodybuilding.com/showthrea … =114052401

I’m currently using Sustain Alpha (mentioned in the thread) and it’s helped a bit, but nothing crazy. Though I haven’t yet had my testosterone/LH tested since taking it.

Also from that thread this nugget of gold:

“Acta Endocrinol (Copenh). 1983 Aug;103(4):451-6.Links
GABA-ergic and dopaminergic mechanisms in gonadotrophin secretion in males–effects of baclofen and metoclopramide.Elias AN, Szekeres AV, Stone S, Valenta LJ, Haw T, Ascher MS.
The GABA analogue, baclofen, and the dopamine antagonist, metoclopramide, were studied with respect to their effects on basal and LRH-induced LH and FSH release in 6 normal male volunteers. Basal gonadotrophin secretion was unchanged following the administration of baclofen or metoclopramide given alone or in combination. LRH-stimulated LH release was significantly blunted after metoclopramide administration in the baclofen pre-treated volunteers. Serum LH concentration (mean +/- SD) in the control phase was 30.1 +/- 17.2 mIU/ml and was 19.4 +/- 9.6 mIU/ml after baclofen plus metoclopramide (P less than 0.02). LRH-stimulated values, however, were unaffected by baclofen or metoclopramide when the drugs were given alone. LRH-stimulated FSH release was not significantly influenced by baclofen or metoclopramide given alone or in combination. Basal Prl secretion increased significantly when baclofen and metoclopramide were given separately and in combination. Basal Prl concentration (mean +/- SD) increased from 14 +/- 2 ng/ml to 18.7 +/- 4.8 ng/ml after baclofen and to 111.5 +/- 31.9 ng/ml after metoclopramide (P less than 0.01). The rise in serum Prl concentration, however, was not significantly different when measured after metoclopramide alone (111 +/- 31.9 ng/ml) or after metoclopramide and baclofen (112 +/- 33.3 ng/ml). It is proposed that GABA and dopamine exert opposing effects on LH secretion in normal men.”

Also:

“Five clinically normal male volunteers were given metoclopramide, 10 mg t.d.s. for 6 weeks. During treatment prolactin concentrations were elevated (over 50 ng/ml) in all. LH, FSH, testosterone and cortisol concentrations were not altered. No change was observed in LH or FSH responses to LHRH testing 4 weeks after the beginning of therapy, compared with pre-treatment values. A reduction in seminal volume and total sperm count were observed in each subject. Four noticed a decrease in libido and three lost spontaneous erections. While the metoclopramide-induced hyperprolactinaemia could be the cause of the observed changes in semen and erectile activity, it is possible that this dopamine receptor blocking drug might directly affect central or peripheral mechanism of erection, the testes or accessory organs.”

Source: www3.interscience.wiley.com/jour … 1&SRETRY=0

Looks like dopamine plays a big role in erections possibly independant of testosterone.

Also right from the devil itself:

Hypogonadism - Secondary (hypothalamic-pituitary) - Acquired causes: metoclopramide
merck.com/mmpe/sec17/ch227/ch227b.html