[ Pobierz całość w formacie PDF ]
Columns were washed with 10 mL of 5 mM myo-inositol and
coupling reaction of organoboron compounds with organic tri-
10 mL of 5 mM sodium borate/60 mM sodium formate. Total
flates. J. Org. Chem. 1993, 58, 2201-2208.
IPs were eluted with 3 mL of 0.1 M formic acid/1 M ammonium
(15) Ho, B. T.; McIsaac, W. M.; An, R.; Tansey, L. W.; Walker, K. E.;
formate. Radioactivity was measured by liquid scintillation Englert, L. F., Jr.; Noel, M. B. Analogues of R-methylphenethyl-
counting in Ecoscint cocktail. Assays were performed in amine (amphetamine). I. Synthesis and pharmacological activity
of some methoxy and/or methyl analogues. J. Am. Chem. Soc.
triplicate.
1970, 13, 26-30.
(16) Barfknecht, C. F.; Nichols, D. E. Potential Psychotomimetics.
Acknowledgment. This work was supported in part
Bromomethoxyamphetamines. J. Med. Chem. 1971, 14, 370-
by PHS grant DA-01642 (R.A.G.), MH 56650 (M.T.), and
372.
MH 57019 (K.H.D.). The authors thank Dr. J. De Los
(17) Nichols, D. E.; Frescas, S.; Marona-Lewicka, D.; Huang, X.; Roth,
Angeles for his assistance with the synthesis of com-
B. L.; Gudelsky, G. A.; Nash, J. F. 1-(2,5-Dimethoxy-4-trifluo-
pound 9 and Dr. Mark Seggel for the synthesis of romethyl)phenyl)-2-aminopropane: A Potent Serotonin 5-HT2A/2C
Agonist. J. Med. Chem. 1994, 37, 4346-4351.
compound 10. C.S.D. was the recipient of an AFPE
(18) Metwally, K. A.; Dukat, M.; Egan, C. T.; Smith, C.; DuPre, A.;
Fellowship.
Gauthier, C. B.; Herrick-Davis, K.; Teitler, M.; Glennon, R. A.
Spiperone: influence of spiro ring substituents on 5-HT2A
Supporting Information Available: Elemental analysis.
serotonin receptor binding. J. Med. Chem. 1998, 41, 5084-5093.
This material is available free of charge via the Internet at
(19) Cheng, Y.-C.; Prusoff, W. H. Relationship between inhibitory
http://pubs.acs.org.
constant (Ki) and the concentration of inhibitor which causes
50% inhibition (IC50) of an enzyme reaction. Biochem. Phar-
References
macol. 1973, 22, 3099-3108.
(20) Herrick-Davis, K.; Egan, C. T.; Teitler, M. Activating mutations
(1) Hoyer, D.; Clarke, D. E.; Fozard, J. R.; Hartig, P. R.; Martin, G.
of the serotonin 5-HT2C receptor. J. Neurochem. 1997, 69,
R.; Mylecharane, E. J.; Saxena, P. R.; Humphrey, P. P. A.
International Union of Pharmacology classification of receptors 1138-1144.
for 5-hydroxytryptamine (serotonin). Pharmacol. Rev. 1994, 46,
157-203. JM9906062 [ Pobierz całość w formacie PDF ]
zanotowane.pl doc.pisz.pl pdf.pisz.pl fopke.keep.pl
Columns were washed with 10 mL of 5 mM myo-inositol and
coupling reaction of organoboron compounds with organic tri-
10 mL of 5 mM sodium borate/60 mM sodium formate. Total
flates. J. Org. Chem. 1993, 58, 2201-2208.
IPs were eluted with 3 mL of 0.1 M formic acid/1 M ammonium
(15) Ho, B. T.; McIsaac, W. M.; An, R.; Tansey, L. W.; Walker, K. E.;
formate. Radioactivity was measured by liquid scintillation Englert, L. F., Jr.; Noel, M. B. Analogues of R-methylphenethyl-
counting in Ecoscint cocktail. Assays were performed in amine (amphetamine). I. Synthesis and pharmacological activity
of some methoxy and/or methyl analogues. J. Am. Chem. Soc.
triplicate.
1970, 13, 26-30.
(16) Barfknecht, C. F.; Nichols, D. E. Potential Psychotomimetics.
Acknowledgment. This work was supported in part
Bromomethoxyamphetamines. J. Med. Chem. 1971, 14, 370-
by PHS grant DA-01642 (R.A.G.), MH 56650 (M.T.), and
372.
MH 57019 (K.H.D.). The authors thank Dr. J. De Los
(17) Nichols, D. E.; Frescas, S.; Marona-Lewicka, D.; Huang, X.; Roth,
Angeles for his assistance with the synthesis of com-
B. L.; Gudelsky, G. A.; Nash, J. F. 1-(2,5-Dimethoxy-4-trifluo-
pound 9 and Dr. Mark Seggel for the synthesis of romethyl)phenyl)-2-aminopropane: A Potent Serotonin 5-HT2A/2C
Agonist. J. Med. Chem. 1994, 37, 4346-4351.
compound 10. C.S.D. was the recipient of an AFPE
(18) Metwally, K. A.; Dukat, M.; Egan, C. T.; Smith, C.; DuPre, A.;
Fellowship.
Gauthier, C. B.; Herrick-Davis, K.; Teitler, M.; Glennon, R. A.
Spiperone: influence of spiro ring substituents on 5-HT2A
Supporting Information Available: Elemental analysis.
serotonin receptor binding. J. Med. Chem. 1998, 41, 5084-5093.
This material is available free of charge via the Internet at
(19) Cheng, Y.-C.; Prusoff, W. H. Relationship between inhibitory
http://pubs.acs.org.
constant (Ki) and the concentration of inhibitor which causes
50% inhibition (IC50) of an enzyme reaction. Biochem. Phar-
References
macol. 1973, 22, 3099-3108.
(20) Herrick-Davis, K.; Egan, C. T.; Teitler, M. Activating mutations
(1) Hoyer, D.; Clarke, D. E.; Fozard, J. R.; Hartig, P. R.; Martin, G.
of the serotonin 5-HT2C receptor. J. Neurochem. 1997, 69,
R.; Mylecharane, E. J.; Saxena, P. R.; Humphrey, P. P. A.
International Union of Pharmacology classification of receptors 1138-1144.
for 5-hydroxytryptamine (serotonin). Pharmacol. Rev. 1994, 46,
157-203. JM9906062 [ Pobierz całość w formacie PDF ]