Giza
Ex-Bluelighter
What is femtomolar range?
in the femtomolar range causing inhibition
in the femtomolar range causing inhibition
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N&PD Moderators: Skorpio | someguyontheinternet
femtomolar range??
- Thread starter Giza
- Start date
Grignard
Bluelighter
10 to the minus 15th Molar, otherwise known as a very, very, very tiny concentration of material
Giza
Ex-Bluelighter
so 'molar' basically = purity of active in X amount of material wether liquid, powder, etc?
Like I dont understand what Molar really means... something active in the femtomolar, would mean its, assuming somone had receptor grade material thats very pure, active in the nanograms? Or would that be even LOWER than nanograms?
And since ive never known beyond nanograms, theres 1000 nanograms in 1mcg yes? So what is the 'name' for the 'grams' below nanograms?
Like I dont understand what Molar really means... something active in the femtomolar, would mean its, assuming somone had receptor grade material thats very pure, active in the nanograms? Or would that be even LOWER than nanograms?
And since ive never known beyond nanograms, theres 1000 nanograms in 1mcg yes? So what is the 'name' for the 'grams' below nanograms?
Grignard
Bluelighter
Molarity = moles of substance/liters of solution, i.e. a 1 molar solution is equivalent to having 1 mole of some compound dissolved in 1 liter of solution(or 0.1 moles of substance dissolved in 100 mL of solution, etc.)
So if you have a 1 femtomolar solution of something it means that you have 1 x 10 to the minus 15th moles of that substance per liter of solution. It really has nothing to do with purity of a material, just the concentration of it.
Also for the various orders of magnitude see this page.
So if you have a 1 femtomolar solution of something it means that you have 1 x 10 to the minus 15th moles of that substance per liter of solution. It really has nothing to do with purity of a material, just the concentration of it.
Also for the various orders of magnitude see this page.
phase_dancer
Bluelight Crew
.. and just to expand on that a bit in case a mole still sounds more like a creature that lives in a hole rather than a scientific measurement..
1 mole of a substance is it's molecular weight. 1 mole of H2O = ~18 grams, calculated by adding the atomic weights of oxygen (O =16 grams) to 2 x hydrogen (H= 1.0079g). Likewise, a substance such as MDMA HCl that has a molecular formula of C11H15NO2.HCl has a molecular weight of 229.71 grams
1 mole of a substance is it's molecular weight. 1 mole of H2O = ~18 grams, calculated by adding the atomic weights of oxygen (O =16 grams) to 2 x hydrogen (H= 1.0079g). Likewise, a substance such as MDMA HCl that has a molecular formula of C11H15NO2.HCl has a molecular weight of 229.71 grams
Giza
Ex-Bluelighter
okay I really wanna grasp this subject so bare with me...
so something in the femtomolar range would be point something of the molecular weight of that particular chemical, point what (i.e; 0.00001) would FEMTOmolar be?
And in the bolded statement at the start of topic, would mean that it causes inhibition at a mole/liter concentration in the femotmolar range??
and how would one derive a nanogram/kg dosing system from such information?
so something in the femtomolar range would be point something of the molecular weight of that particular chemical, point what (i.e; 0.00001) would FEMTOmolar be?
And in the bolded statement at the start of topic, would mean that it causes inhibition at a mole/liter concentration in the femotmolar range??
and how would one derive a nanogram/kg dosing system from such information?
BilZ0r
Bluelight Crew
- Joined
- Dec 15, 2003
- Messages
- 6,675
femtomolar would be 0.000000000000001 moles per letre.
To convert that to a weight you need to know the molecular weight of the compound in question (measured in grams per mole). The weight in grams = molecular mass times number of moles.
But of course, you're trying to convert a concentration in an in vitro system, to a dose, in an in vivo system. Which you can't do, unless you know fuck loads of information about how a drug is absorbed, distributed and metabolized.
To convert that to a weight you need to know the molecular weight of the compound in question (measured in grams per mole). The weight in grams = molecular mass times number of moles.
But of course, you're trying to convert a concentration in an in vitro system, to a dose, in an in vivo system. Which you can't do, unless you know fuck loads of information about how a drug is absorbed, distributed and metabolized.
Giza
Ex-Bluelighter
Well there is in vivo mouse and rhesus monkey studies regarding it, and both revealed similar potencies, although it failed to list the actual dosage being used in the abstract. But the femtomolar shit was brought up in regards to a mouse MVD preparation, which im assuming means an in vitro cell culture of MVD cells.
But still, I dont know if its possible. But if you have a better way to find out a rough number of where to start human trials at based on mouse and monkey studies id love to hear it, otherwise this is about the only way... better stock up on the naloxone.
But still, I dont know if its possible. But if you have a better way to find out a rough number of where to start human trials at based on mouse and monkey studies id love to hear it, otherwise this is about the only way... better stock up on the naloxone.
Giza
Ex-Bluelighter
^ If you can get a hold of em... please share 
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.
Brine GA, Stark PA, Liu Y, Carroll FI, Singh P, Xu H, Rothman RB.
Research Triangle Institute, Research Triangle Park, North Carolina 27709, USA.
Abstract
(+/-)-cis-N-[1-(2-Hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]-N- phenylpropanamide (1) is a mixture of four stereoisomers [(2S,3R,4S)-1a, (2R,3R,4S)-1b, (2R,3S,4R)-1c, and (2S,3S,4R)-1d], which together constitute two diastereoisomeric pairs of optical isomers. These four stereoisomers were prepared from optically active intermediates of known absolute configuration by procedures which had no effect on the configurations of the piperidine 3- and 4-carbons. The configuration of the phenylethyl 2-carbon in the final products was determined by X-ray analysis of (2S,3S,4R)-1d. A 1H NMR comparison of the final products to ohmefentanyl established that the racemic pair previously known as ohmefentanyl was a mixture of (2S,3R,4S)-1a and (2R,3S,4R)-1c. The individual activities of 1a, 1b, 1c, and 1d were evaluated in a variety of binding and pharmacological assays. The binding data revealed that isomers 1b and 1c had the highest affinity and selectivity for the mu site labeled with [3H]DAMGO. In contrast, the four isomers displaced [3H]etorphine in the order 1a approximately 1b > 1c approximately 1d. Evaluation of the four isomers on the mouse vas deferens (MVD) preparation revealed a potency order of 1a > 1b > 1c > 1d with concentrations of 1a and 1b in the femtomolar range causing inhibition. Experiments using the antagonists naltrexone (mu), ICI 174864 (delta), and norbinaltorphimine (kappa) demonstrated that the effects of 1a were mediated largely by the mu receptor while both delta and kappa agonist effects contributed to the actions of 1b and 1c. Isomer 1d acted as a weak mu antagonist in the MVD preparation. The same potency order was observed in a mouse analgesic assay and a rhesus monkey single dose suppression study. From the latter study the potency of 1a was estimated to be 20,000-50,000 times that of morphine, making this isomer one of the most potent opiates known. In the rhesus monkey study, isomer 1d failed to substitute for morphine and seemed to exacerbate withdrawal at doses of 0.6, 3.0, and 6.0 mg/kg. On the basis of the mouse data, isomer 1a was 21,000 times more potent than 1d, whereas isomers 1b and 1c were similar in their opiate activity in vivo. Using the optical isomers of cis-3-methylfentanyl as reference compounds, we analyzed the effects on the pharmacological activities of introducing a phenylethyl 2-hydroxyl group into the molecule.
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.
Brine GA, Stark PA, Liu Y, Carroll FI, Singh P, Xu H, Rothman RB.
Research Triangle Institute, Research Triangle Park, North Carolina 27709, USA.
Abstract
(+/-)-cis-N-[1-(2-Hydroxy-2-phenylethyl)-3-methyl-4-piperidyl]-N- phenylpropanamide (1) is a mixture of four stereoisomers [(2S,3R,4S)-1a, (2R,3R,4S)-1b, (2R,3S,4R)-1c, and (2S,3S,4R)-1d], which together constitute two diastereoisomeric pairs of optical isomers. These four stereoisomers were prepared from optically active intermediates of known absolute configuration by procedures which had no effect on the configurations of the piperidine 3- and 4-carbons. The configuration of the phenylethyl 2-carbon in the final products was determined by X-ray analysis of (2S,3S,4R)-1d. A 1H NMR comparison of the final products to ohmefentanyl established that the racemic pair previously known as ohmefentanyl was a mixture of (2S,3R,4S)-1a and (2R,3S,4R)-1c. The individual activities of 1a, 1b, 1c, and 1d were evaluated in a variety of binding and pharmacological assays. The binding data revealed that isomers 1b and 1c had the highest affinity and selectivity for the mu site labeled with [3H]DAMGO. In contrast, the four isomers displaced [3H]etorphine in the order 1a approximately 1b > 1c approximately 1d. Evaluation of the four isomers on the mouse vas deferens (MVD) preparation revealed a potency order of 1a > 1b > 1c > 1d with concentrations of 1a and 1b in the femtomolar range causing inhibition. Experiments using the antagonists naltrexone (mu), ICI 174864 (delta), and norbinaltorphimine (kappa) demonstrated that the effects of 1a were mediated largely by the mu receptor while both delta and kappa agonist effects contributed to the actions of 1b and 1c. Isomer 1d acted as a weak mu antagonist in the MVD preparation. The same potency order was observed in a mouse analgesic assay and a rhesus monkey single dose suppression study. From the latter study the potency of 1a was estimated to be 20,000-50,000 times that of morphine, making this isomer one of the most potent opiates known. In the rhesus monkey study, isomer 1d failed to substitute for morphine and seemed to exacerbate withdrawal at doses of 0.6, 3.0, and 6.0 mg/kg. On the basis of the mouse data, isomer 1a was 21,000 times more potent than 1d, whereas isomers 1b and 1c were similar in their opiate activity in vivo. Using the optical isomers of cis-3-methylfentanyl as reference compounds, we analyzed the effects on the pharmacological activities of introducing a phenylethyl 2-hydroxyl group into the molecule.