("alpha-adrenergic technology")
Bioorg Med Chem Lett 2000 Jan 17;10(2):175-8
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.
Lagu B, Tian D, Chiu G, Nagarathnam D, Fang J, Shen Q, Forray C, Ransom RW, Chang RS, Vyas KP, Zhang K, Gluchowski C
Department of Chemistry, Synaptic Pharmaceutical Corporation, Paramus, NJ 07652, USA.
Furo[3,4-d]pyrimidinones were found to be metabolites of dihydropyrimidinones such as 1a-b that are subtype-selective antagonists of the alpha1a-adrenergic receptor. A versatile synthesis that provides access to furo[3,4-d]pyrimidinones in high yield and in enantiomerically pure forms is described along with structure-activity relationships in the series.
PMID: 10673105, UI: 20135660
(hand on chin, ah yes, I see <guffaw>)
A more recent abstract:
Trends Pharmacol Sci 2000 Mar;21(3):109-117
Galanin receptor subtypes.
Branchek TA, Smith KE, Gerald I, Walker MW
Synaptic Pharmaceutical Corporation, 215 College Road, Paramus, NJ 07652, USA.
The neuropeptide galanin, which is widely expressed in brain and peripheral tissues, exerts a broad range of physiological effects. Pharmacological studies using peptide analogues have led to speculation about multiple galanin receptor subtypes. Since 1994, a total of three G-protein-coupled receptor (GPCR) subtypes for galanin have been cloned (GAL1, gal2 and gal3). Potent, selective antagonists are yet to be found for any of the cloned receptors. Major challenges in this field include linking the receptor clones with each of the known physiological actions of galanin and evaluating the evidence for additional galanin receptor subtypes.
PMID: 10689365
and another "alpha-adrenergic"
J Med Chem 1999 Nov 18;42(23):4804-13
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.
Wong WC, Sun W, Lagu B, Tian D, Marzabadi MR, Zhang F, Nagarathnam D, Miao SW, Wetzel JM, Peng J, Forray C, Chang RS, Chen TB, Ransom R, O'Malley S, Broten TP, Kling P, Vyas KP, Zhang K, Gluchowski C
Departments of Chemistry and Pharmacology, Synaptic Pharmaceutical Corporation, Paramus, NJ 07652, USA.
We have previously disclosed dihydropyridines such as 1a,b as selective alpha(1a) antagonists as a potential treatment for benign prostatic hyperplasia (BPH). The propensity of dihydropyridines toward an oxidation led us to find suitable replacements of the core unit. The accompanying papers describe the structure-activity relationship (SAR) of dihydropyrimidinones 2a,b as selective alpha(1a) antagonists. We report herein the SAR of dihydropyrimidines such as 4 and highlight the similarities and differences between the dihydropyrimidine and dihydropyrimidinone series of compounds.
PMID: 10579843, UI: 20048248
and an older post summarizing molecules
Message 11217955
1999 was not a good year for SNAP, maybe their time is coming in 2000, or later. During the last few days the
shareprice action looks very odd--maybe it is some of
that "working the order".
quote.yahoo.com
Will ask about that on one of the share analysis threads. |
