| dc.contributor.advisor |
Rusterholz, David |
|
| dc.contributor.author |
Held, Victoria |
|
| dc.date.accessioned |
2006-09-14T22:04:57Z |
|
| dc.date.available |
2006-09-14T22:04:57Z |
|
| dc.date.issued |
2006-02 |
|
| dc.identifier.citation |
Held, Victoria D. "Design and Synthesis of TRPV1 Antagonists; Probing the D-Region Binding Site Using Amidoalkyl Substituents." Endeavor 2.1 (2006): 27-40. |
en |
| dc.identifier.uri |
http://digital.library.wisc.edu/1793/6778 |
|
| dc.description |
14 p. |
en |
| dc.description.abstract |
Transient receptor potential vanilloid subfamily 1 (TRPV1) is a membrane bound ion channel that mediates the pain response elicited by capsaicin, resiniferatoxin, and similar drugs. Structure activity studies of compounds that bind to TRPV1 indicate several binding sites, namely: 1) an aromatic “A” region, 2) a polar “B” region, and 3) a hydrophobic “C” region. A fourth region has recently been proposed based on the structure of resiniferatoxin. This “D” region is thought to be responsible for the increased potency of the drug. A new series of potential TRPV1 antagonists was designed incorporating molecular features intended to interact with the known A, B, and C binding sites. In order to investigate the interaction of the D binding region, amidoalkyl groups were incorporated into the target structures. The synthesis of several members of the target series was accomplished using a convergent synthetic strategy. Ultimately these compounds will be tested for their effectiveness as TRPV1 antagonists. |
en |
| dc.description.provenance |
Submitted by Heidi J. Southworth (heidi.southworth@uwrf.edu) on 2006-09-14T22:03:58Z
No. of bitstreams: 1
Held.pdf: 156570 bytes, checksum: 242899fb38ad20c2b0de950c5c403f4f (MD5) |
en |
| dc.description.provenance |
Approved for entry into archive by Heidi J. Southworth(heidi.southworth@uwrf.edu) on 2006-09-14T22:04:57Z (GMT) No. of bitstreams: 1
Held.pdf: 156570 bytes, checksum: 242899fb38ad20c2b0de950c5c403f4f (MD5) |
en |
| dc.description.provenance |
Made available in DSpace on 2006-09-14T22:04:57Z (GMT). No. of bitstreams: 1
Held.pdf: 156570 bytes, checksum: 242899fb38ad20c2b0de950c5c403f4f (MD5)
Previous issue date: 2006-02 |
en |
| dc.format.extent |
156570 bytes |
|
| dc.format.mimetype |
application/pdf |
|
| dc.language.iso |
en_US |
en |
| dc.publisher |
University of Wisconsin-River Falls |
en |
| dc.subject |
Transient receptor potential vanilloid subfamily 1 |
en |
| dc.subject |
TRPV1 |
en |
| dc.subject |
TRPV1 antagonists |
en |
| dc.subject |
Binding region |
en |
| dc.subject |
Amidoalkyl substituents |
en |
| dc.subject |
Capsaicin |
en |
| dc.subject |
Receptors |
en |
| dc.subject |
Vanilloids |
en |
| dc.subject |
Article |
en |
| dc.title |
Design and Synthesis of TRPV1 Antagonists; Probing the D-Region Binding Site Using Amidoalkyl Substituents |
en |
| dc.type |
Article |
en |
