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5 results on '"Parmar, Rupa M."'

1. Rapid Identification of Subtype-Selective Agonists of the Somatostatin Receptor Through Combinatorial Chemistry

Author

Rohrer, Susan P., Birzin, Elizabeth T., Mosley, Ralph T., Berk, Scott C., Hutchins, Steven M., Shen, Dong-Ming, Xiong, Yusheng, Hayes, Edward C., Parmar, Rupa M., Foor, Forrest, Mitra, Sudha W., Degrado, Sylvia J., Shu, Min, Klopp, John M., Cai, Sheng-Jian, Blake, Allan, Pasternak, Alex, Yang, Lihu, Patchett, Arthur A., Smith, Roy G., Chapman, Kevin T., and Schaeffer, James M.

Published
1998

2. Synthesis and Biological Activities of Potent Peptidomimetics Selective for Somatostatin Receptor Subtype 2

Author

Yang, Lihu, Berk, Scott C., Rohrer, Susan P., Mosley, Ralph T., Guo, Liangqin, Underwood, Dennis J., Arison, Byron H., Birzin, Elizabeth T., Hayes, Edward C., Mitra, Sudha W., Parmar, Rupa M., Cheng, Kang, Wu, Tsuei-Ju, Butler, Bridgette S., Foor, Forrest, Pasternak, Alexander, Pan, Yanping, Silva, Maria, Freidinger, Roger M., Smith, Roy G., Chapman, Kevin, Schaeffer, James M., and Patchett, Arthur A.

Published
1998

3. Synthesis nd biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2

Author

Yang, Lihu, Berk, Scott C., Rohrer, Susan P., Mosley, Ralph T., Guo, Liangqin, Underwood, dennis J., Arison, Byron H., Birzin, Elizabeth T., Hayes, Edward C., Mitra, Sudha W., Parmar, Rupa M., Cheng, Kang, Wu, Tsuei-ju, Butler. Bridgette S., Foor, Forrest, Pasternak, Alexander, Pan, Yanping, Silva, Maria, Freidinger, Roger M., Smith, Roy G., Chapman, Kevin, Schaeffer, Jmes M., and Patchett, Arthur A.

Subjects
Octreotide acetate -- Research, Rats -- Research, Proteins -- Receptors, Science and technology
Abstract

A series of nonpeptide somatostatin agonists which bind selectively and with high affinity to somatostatin receptor subtype 2 (sst2) have been synthesized. One of these compounds, L-054,522, binds to human sst2 with an apparent dissociation constant of 0.01 nM and at least 3,000-fold selectivity when evaluated against the other somatostatin receptors. L-054,522 is a full agonist based on its inhibition of forskolin-stimulated adenylate cyclase activity in Chinese hamster ovary-K1 cells stably expressing sst2. L-054,522 has a potent inhibitory effect on growth hormone release from rat primary pituitary cells and glucagon release from isolated mouse pancreatic islets. Intravenous infusion of L-054,522 to rats at 50 [[micro]gram]/kg per hr causes a rapid and sustained reduction in growth hormone to basal levels. The high potency and selectivity of L-054,522 for sst2 will make it a useful tool to further characterize the physiological functions of this receptor subtype.

Published
1998

5. Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues

Author

Ye, Zhixiong, primary, Gao, Yingduo, additional, Bakshi, Raman K., additional, Chen, Meng-Hsin, additional, Rohrer, Susan P., additional, Feighner, Scott D., additional, Pong, Sheng-Shung, additional, Howard, Andrew D., additional, Blake, Allan, additional, Birzin, Elizabeth T., additional, Locco, Louis, additional, Parmar, Rupa M., additional, Chan, Wanda W.-S., additional, Schaeffer, James M., additional, Smith, Roy G., additional, Patchett, Arthur A., additional, and Nargund, Ravi P., additional

Published
2000
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