11-Hydroxy-Yohimbine - Halflife = longer but does it block A2 adrenergic equal to YO?

[600538411]

OK so 11-Hydroxy-Yohimbine has a half-life 4 times longer than conventional Yohimbine as pre the following study

Originally Posted by Some Nerds lol

Le Corre P; Dollo G; Chevanne F; Le Verge R
Laboratoire de Pharmacie Gal?nique, Biopharmacie et Pharmacie Clinique, Facult? des Sciences Pharmaceutiques et Biologiques, Universit? de Rennes 1, 35043, Rennes, France. pascal.le-corre@univ-rennes1.fr

The biopharmaceutics of yohimbine (YO) and the pharmacokinetics of 10-hydroxy-yohimbine (10-OH-YO) and 11-hydroxy-yohimbine (11-OH-YO) were investigated in healthy subjects following i.v. (5 mg) and oral (8 mg) dosing. One subject was found as a slow hydroxylator of YO. The mean (+/-S.D.) oral absolute bioavailability of YO was 22.3+/-21. 5%. Total plasma clearance (CL) and renal clearance (CL(r)) of YO following i.v. dosing were 0.728+/-0.256 ml/min and 0.001+/-0.002 ml/min, respectively. Based on the steady-state volume of distribution (V(ss)), YO had a relatively low distribution (V(ss) = 32.2+/-12.1 l). The overall renal excretion of YO, 10-OH-YO and 11-OH-YO, expressed as percent of the dose of YO administered, were not different following i.v. and oral dosing, and were around 0.1, 0.2 and 14%, respectively. Following i.v. dosing of YO, the mean apparent terminal half-life of 11-OH-YO (347+/-63 min) was almost four times higher than that of YO (91.0+/-33.6 min) suggesting an elimination rate-limited kinetics for 11-OH-YO.

But what about it's ability to block the alpha-2 adrenergic receptor? Is it comparable, less, more? anyone have any studies or info to contribute?

[ElMariachi]

Bumping this....up in here...up in here.

[Bane]

It has the same capacity for a2 blockage. It also binds to plasma globulins about 50% less, meaning half the dose to have the same pharmacological effect but also lower half life(much faster clearence)

P.S. Personally I hate Yohimbines

[cakedonkey]

Originally Posted by Bane

P.S. Personally I hate Yohimbines

Same here. Despite true potential for fat burning application, the stuff makes me feel like dying. In other words, potential results are simply not worth the side-effects. I can literally see my heart beating out of my chest using the stuff--it's scary. Downright horrible.

[Vipersg123]

see I've never had an issue with yohimbine... I took primaforce yohimbine HCL 4 caps at one time and still felt nothing.

[Incinerated]

Originally Posted by Vipersg123

see I've never had an issue with yohimbine... I took primaforce yohimbine HCL 4 caps at one time and still felt nothing.

if you take it within 30minutes of carbs it has no effect...