Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity
Тип публикации: Journal Article
Дата публикации: 2007-12-21
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
18095642
Drug Discovery
Molecular Medicine
Краткое описание
The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [(3)H]phosphoinositol turnover: 5-HT2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). Lorcaserin was further characterized in a single-dose pharmacokinetic study in rat (t1/2 = 3.7 h; F = 86%) and a 28-day model of weight gain in growing Sprague-Dawley rat (8.5% decrease in weight gain observed at 36 mg/kg b.i.d.). Lorcaserin was selected for further evaluation in clinical trials for the treatment of obesity.
Найдено
Ничего не найдено, попробуйте изменить настройки фильтра.
Для доступа к списку цитирований публикации необходимо авторизоваться.
Для доступа к списку профилей, цитирующих публикацию, необходимо авторизоваться.
Топ-30
Журналы
|
2
4
6
8
10
12
14
|
|
|
Bioorganic and Medicinal Chemistry Letters
13 публикаций, 7.51%
|
|
|
Organic Letters
9 публикаций, 5.2%
|
|
|
Journal of Medicinal Chemistry
7 публикаций, 4.05%
|
|
|
Psychopharmacology
4 публикации, 2.31%
|
|
|
Tetrahedron Asymmetry
4 публикации, 2.31%
|
|
|
Bioorganic and Medicinal Chemistry
4 публикации, 2.31%
|
|
|
ACS Chemical Neuroscience
4 публикации, 2.31%
|
|
|
Journal of Pharmacology and Experimental Therapeutics
3 публикации, 1.73%
|
|
|
Tetrahedron
3 публикации, 1.73%
|
|
|
Neuropharmacology
3 публикации, 1.73%
|
|
|
Organometallics
3 публикации, 1.73%
|
|
|
ACS Catalysis
3 публикации, 1.73%
|
|
|
Pharmacology and Therapeutics
2 публикации, 1.16%
|
|
|
European Journal of Medicinal Chemistry
2 публикации, 1.16%
|
|
|
Life Sciences
2 публикации, 1.16%
|
|
|
ChemMedChem
2 публикации, 1.16%
|
|
|
Chinese Journal of Chemistry
2 публикации, 1.16%
|
|
|
Pharmacology Research and Perspectives
2 публикации, 1.16%
|
|
|
Chemistry - A European Journal
2 публикации, 1.16%
|
|
|
Organic Process Research and Development
2 публикации, 1.16%
|
|
|
Organic and Biomolecular Chemistry
2 публикации, 1.16%
|
|
|
RSC Advances
2 публикации, 1.16%
|
|
|
Expert Review of Clinical Pharmacology
2 публикации, 1.16%
|
|
|
Drug Metabolism and Disposition
1 публикация, 0.58%
|
|
|
Current Microwave Chemistry
1 публикация, 0.58%
|
|
|
Current Pharmaceutical Design
1 публикация, 0.58%
|
|
|
Journal of Clinical Endocrinology and Metabolism
1 публикация, 0.58%
|
|
|
Journal of Medicinal Food
1 публикация, 0.58%
|
|
|
New England Journal of Medicine
1 публикация, 0.58%
|
|
|
2
4
6
8
10
12
14
|
Издатели
|
10
20
30
40
50
60
|
|
|
Elsevier
54 публикации, 31.21%
|
|
|
American Chemical Society (ACS)
32 публикации, 18.5%
|
|
|
Wiley
24 публикации, 13.87%
|
|
|
Springer Nature
14 публикаций, 8.09%
|
|
|
Taylor & Francis
9 публикаций, 5.2%
|
|
|
Royal Society of Chemistry (RSC)
8 публикаций, 4.62%
|
|
|
American Society for Pharmacology and Experimental Therapeutics
4 публикации, 2.31%
|
|
|
Bentham Science Publishers Ltd.
3 публикации, 1.73%
|
|
|
Ovid Technologies (Wolters Kluwer Health)
3 публикации, 1.73%
|
|
|
SAGE
3 публикации, 1.73%
|
|
|
MDPI
2 публикации, 1.16%
|
|
|
The Endocrine Society
1 публикация, 0.58%
|
|
|
Mary Ann Liebert
1 публикация, 0.58%
|
|
|
Massachusetts Medical Society
1 публикация, 0.58%
|
|
|
Japanese Society of Internal Medicine
1 публикация, 0.58%
|
|
|
Frontiers Media S.A.
1 публикация, 0.58%
|
|
|
OOO Zhurnal "Mendeleevskie Soobshcheniya"
1 публикация, 0.58%
|
|
|
Federation of American Societies for Experimental Biology (FASEB)
1 публикация, 0.58%
|
|
|
Korean Diabetes Association
1 публикация, 0.58%
|
|
|
American Society of Health-System Pharmacists
1 публикация, 0.58%
|
|
|
Oxford University Press
1 публикация, 0.58%
|
|
|
American Association for the Advancement of Science (AAAS)
1 публикация, 0.58%
|
|
|
Annual Reviews
1 публикация, 0.58%
|
|
|
Georg Thieme Verlag KG
1 публикация, 0.58%
|
|
|
BMJ
1 публикация, 0.58%
|
|
|
National Academy of Sciences of Ukraine (Co. LTD Ukrinformnauka) (Publications)
1 публикация, 0.58%
|
|
|
10
20
30
40
50
60
|
- Мы не учитываем публикации, у которых нет DOI.
- Статистика публикаций обновляется еженедельно.
Вы ученый?
Создайте профиль, чтобы получать персональные рекомендации коллег, конференций и новых статей.
Метрики
173
Всего цитирований:
173
Цитирований c 2025:
4
(2.31%)
Цитировать
ГОСТ |
RIS |
BibTex |
MLA
Цитировать
ГОСТ
Скопировать
Smith B. M. et al. Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity // Journal of Medicinal Chemistry. 2007. Vol. 51. No. 2. pp. 305-313.
ГОСТ со всеми авторами (до 50)
Скопировать
Smith B. M., Smith J. M., Tsai J. H., Schultz J., Gilson C. A., Estrada S. A., Chen R. R., Park D. M., Prieto E. B., Gallardo C. S., Sengupta D., Dosa P. I., Covel J. A., Ren A., Webb R. R., Beeley N. R., Martin M., Morgan M., Espitia S., Saldana H. R., Bjenning C., Whelan K. T., Grottick A. J., Menzaghi F., Thomsen W. J. Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity // Journal of Medicinal Chemistry. 2007. Vol. 51. No. 2. pp. 305-313.
Цитировать
RIS
Скопировать
TY - JOUR
DO - 10.1021/jm0709034
UR - https://doi.org/10.1021/jm0709034
TI - Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity
T2 - Journal of Medicinal Chemistry
AU - Smith, Brian M.
AU - Smith, Jeffrey M.
AU - Tsai, James H
AU - Schultz, Jeffrey A.
AU - Gilson, Charles A
AU - Estrada, Scott A
AU - Chen, Rita R
AU - Park, Douglas M
AU - Prieto, Emily B
AU - Gallardo, Charlemagne S
AU - Sengupta, Dipanjan
AU - Dosa, Peter I.
AU - Covel, Jon A
AU - Ren, Albert
AU - Webb, Robert R.
AU - Beeley, Nigel R.A.
AU - Martin, Michael
AU - Morgan, Michael
AU - Espitia, Stephen
AU - Saldana, Hazel R
AU - Bjenning, Christina
AU - Whelan, Kevin T
AU - Grottick, A. J.
AU - Menzaghi, Frédérique
AU - Thomsen, William J.
PY - 2007
DA - 2007/12/21
PB - American Chemical Society (ACS)
SP - 305-313
IS - 2
VL - 51
PMID - 18095642
SN - 0022-2623
SN - 1520-4804
ER -
Цитировать
BibTex (до 50 авторов)
Скопировать
@article{2007_Smith,
author = {Brian M. Smith and Jeffrey M. Smith and James H Tsai and Jeffrey A. Schultz and Charles A Gilson and Scott A Estrada and Rita R Chen and Douglas M Park and Emily B Prieto and Charlemagne S Gallardo and Dipanjan Sengupta and Peter I. Dosa and Jon A Covel and Albert Ren and Robert R. Webb and Nigel R.A. Beeley and Michael Martin and Michael Morgan and Stephen Espitia and Hazel R Saldana and Christina Bjenning and Kevin T Whelan and A. J. Grottick and Frédérique Menzaghi and William J. Thomsen},
title = {Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity},
journal = {Journal of Medicinal Chemistry},
year = {2007},
volume = {51},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/jm0709034},
number = {2},
pages = {305--313},
doi = {10.1021/jm0709034}
}
Цитировать
MLA
Скопировать
Smith, Brian M., et al. “Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity.” Journal of Medicinal Chemistry, vol. 51, no. 2, Dec. 2007, pp. 305-313. https://doi.org/10.1021/jm0709034.