c' est de la MERDE parole de cocaïnomanbe qui se revendique comme tel !
3-Pseudotropyl-4-fluorobenzoate
AKA ,
---4-fluorotropacocaine
---pFBT
--- 8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 4-fluorobenzoic acid ester
IUPAC:
(1R,5S)-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-4-fluorobenzoate
CAS ;
172883-97-5
30% the stimulant potency of cocaine but around the same potency as a local anaesthetic
En gros pour un effet stim comparable , tu crèves d'une vasoconstriction cardiaque avant car ça a aussi des effets vasoconstricteurs peripheripheriques et centraux , pas seulement locaux
C'est DANGEUREUX.
et ca ne touche pas a tes 5HT1 comme la coke le fait , seulement a tes dopaminergiques .
allé un peu de culture (non pas hors sujet justement , extention = compréhension )
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
Agoston GE, Wu JH, Izenwasser S, George C, Katz J, Kline RH, Newman AH.
Psychobiology Section, National Institute on Drug Abuse, National Institutes of Health, Baltimore, Maryland 21224, USA.
A series of N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues has been prepared that function as dopamine uptake inhibitors.
The N-methylated analogue of this series had a significantly higher affinity for the dopamine transporter than the parent compound, N-methyl-3 alpha- (diphenylmethoxy)tropane (benztropine, Cogentin).
Yet like the parent compound, it retained high affinity for muscarinic receptors. A series of N-substituted compounds were prepared from nor-3 alpha-[bis(4'-fluorophenyl)methoxy]tropane via acylation followed by hydride reduction of the amide or by direct alkylation. All compounds containing a basic tropane nitrogen displaced [3H]WIN 35,428 at the dopamine transporter (Ki range = 8.5-634 nM) and blocked dopamine uptake (IC50 range = 10-371 nM) in rat caudate putamen, whereas ligands with a nonbasic nitrogen were virtually inactive.
None of the compounds demonstrated high binding affinity at norepinephrine or serotonin transporters.
Importantly, a separation of binding affinities for the dopamine transporter versus muscarinic m1 receptors was achieved by substitution of the N-methyl group with other N-alkyl or arylalkyl substituents (eg. n-butyl, allyl, benzyl, 3-phenylpropyl, etc.).
Additionally, the most potent and selective analogue in this series at the dopamine transporter, N-(4"-phenyl-n-butyl)-3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogue failed to substitute for cocaine in rats trained to discriminate cocaine from saline.
Potentially, new leads toward the development of a pharmacotherapeutic for cocaine abuse and other disorders affecting the dopamine transporter may be discovered.
PMID: 9435902 [PubMed - indexed for MEDLINE]
pour les curieux qui veulent apprendre par eux même , petite selection sympa :
http://www.ncbi.nlm.nih.gov/pubmed/2755 ... rom=pubmed
http://dx.doi.org/10.1007/s002130000568
http://www.springerlink.com/content/jl27305140p02v87/
http://dx.doi.org/10.1007/BF01936761
http://www.ncbi.nlm.nih.gov/pubmed/1913 ... tlesearch4
http://www.ncbi.nlm.nih.gov/pubmed/8848 ... rom=pubmed
http://chem.sis.nlm.nih.gov/chemidplus/ ... 0000053214
http://www.ncbi.nlm.nih.gov/pubmed/1943051
http://www.ncbi.nlm.nih.gov/pubmed/2755088
http://www.ncbi.nlm.nih.gov/pubmed/7116761
a lire
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