Aimed at achieving a good understanding of the 3-dimensional structures of human alpha1A-adrenoceptor (alpha1A-AR), we have successfully developed its homology model based on the crystal structure of beta2-AR. Subsequent structural refinements were performed to mimic the receptor's natural membrane environment by using molecular mechanics (MM) and molecular dynamics (MD) simulations in the GBSW implicit membrane model. Through molecular docking and further simulations, possible binding modes of subtype-selective alpha1A-AR antagonists, Silodosin, RWJ-69736 and (+)SNAP-7915, were examined. Results of the modeling and docking studies are qualitatively consistent with available experimental data from mutagenesis studies. The homology model built should be very useful for designing more potent subtype-selective alpha1A-AR antagonists and for guiding further mutagenesis studies.

01 Dec 2000·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Determination of the relative and absolute stereochemistry of a potent and α1A-selective adrenoceptor antagonist

Q4 · MEDICINE

Article

Author: Forray, C. ; Bock, M. G. ; Patane, M. A. ; Lagu, B. ; Wetzel, J. M.

The binding affinities and selectivities of antagonists 1-4 for the alpha1A-adrenoceptor are dependent on the stereochemical orientation of the groups at the C-4 and C-5 positions of the oxazolidinone ring. The unambiguous assignment of the relative and absolute configurations of the diastereomers of SNAP 7915 (1) is reported.

01 Jul 2000·Journal of Medicinal ChemistryQ1 · MEDICINE

De Novo Design of a Novel Oxazolidinone Analogue as a Potent and Selective α_1A Adrenergic Receptor Antagonist with High Oral Bioavailability

Q1 · MEDICINE

Article

Author: Pettibone, Douglas J. ; Li, Chao ; Ransom, Richard W. ; Kassahun, Kelem ; Tian, Dake ; Lagu, Bharat ; Gluchowski, Charles ; Chan, Tsing-Bao ; Rodrigues, A. David ; Chang, Raymond S. L. ; Broten, Theodore P. ; O'Malley, Stacey S. ; Shen, Quanrong ; Forray, Carlos ; Wetzel, John M. ; Schorn, Terry W. ; Freidinger, Roger ; Nagarathnam, Dhanapalan ; Jeon, Yoon

This communication describes the synthesis of a novel oxazolidinone, SNAP 7915, and the in vitro and in vivo profile of this compound

100 Deals associated with SNAP-7915

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Prostatic Hyperplasia	Discovery	US	Lundbeck Research USA, Inc.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

SNAP-7915

Overview

Basic Info

Structure

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation