Search Results - "J A Lowe, 3rd"
-
1
Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity
Published in The Journal of pharmacology and experimental therapeutics (01-10-1995)“…Ziprasidone (CP-88,059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects in preclinical assays predictive of…”
Get more information
Journal Article -
2
A Potent Nonpeptide Antagonist of the Substance P (NK$_1$) Receptor
Published in Science (American Association for the Advancement of Science) (25-01-1991)“…CP-96,345 [(2S, 3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)-methyl]-1-azabicyclo[2.2.2] octan-3-amine] is a potent nonpeptide antagonist of the substance P…”
Get full text
Journal Article -
3
Molecular basis for the species selectivity of the substance P antagonist CP-96,345
Published in The Journal of biological chemistry (05-02-1993)“…The non-peptide substance P (SP) antagonist CP-96,345 has a 90-fold selectivity for the human neurokinin-1 (NK-1) or SP receptor over the rat NK-1 receptor,…”
Get full text
Journal Article -
4
Two nonpeptide tachykinin antagonists act through epitopes on corresponding segments of the NK1 and NK2 receptors
Published in Proceedings of the National Academy of Sciences - PNAS (01-07-1993)“…The molecular mechanism of action for two chemically distinct and highly selective, nonpeptide antagonists, CP-96,345 and SR-48,968, was studied by development…”
Get full text
Journal Article -
5
Activity and Distribution of Binding Sites in Brain of a Nonpeptide Substance P (NK$_1$) Receptor Antagonist
Published in Science (American Association for the Advancement of Science) (25-01-1991)“…CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK$_1$ receptor. The compound binds to a single population of sites in guinea…”
Get full text
Journal Article -
6
Selective Inhibition of the Carotid Body Sensory Response to Hypoxia by the Substance P Receptor Antagonist CP-96,345
Published in Proceedings of the National Academy of Sciences - PNAS (01-11-1993)“…Carotid bodies are sensory organs for monitoring arterial oxygen and CO2. Previous studies have shown that chemoreceptor tissue contains substance P (SP) and…”
Get full text
Journal Article Conference Proceeding -
7
Photoaffinity labeling of the human substance P (neurokinin-1) receptor with [3H2]azido-CP-96,345, a photoreactive derivative of a nonpeptide antagonist
Published in Molecular pharmacology (01-05-1996)“…An azido derivative of [3H2](2S, 3S)-cis-2-(diphenylmethyl)-N-((2-methoxyphenyl) methyl)-1-azabicyclo[2.2.2]octon-3-amine (CP-96,345), a potent nonpeptide…”
Get more information
Journal Article -
8
Effect of CP-96,345, a Nonpeptide Substance P Receptor Antagonist, on Salivation in Rats
Published in Proceedings of the National Academy of Sciences - PNAS (15-11-1991)“…CP-96,345 {(2S,3S)-cis-2-(diphenylmethyl)-N-[(2-methoxyphenyl)methyl]-1 -azabicyclo[2.2.2]octa N-3-amine} antagonism of substance P-stimulated salivation was…”
Get full text
Journal Article -
9
Specific residues at the top of transmembrane segment V and VI of the neurokinin-1 receptor involved in binding of the nonpeptide antagonist CP 96,345 [corrected]
Published in The Journal of biological chemistry (30-09-1994)“…Previously we have found that binding of the nonpeptide substance P antagonist, CP 96,345, to the neurokinin-1 (NK-1) receptor was critically dependent on two…”
Get full text
Journal Article -
10
Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist
Published in Nature (London) (25-03-1993)“…Non-peptide ligands for peptide receptors have been discovered in several systems through file screening programs, but the mechanism of action for these…”
Get full text
Journal Article -
11
Effects of the cannabinoid CB1 receptor antagonist SR141716A on the behavior of pigeons and rats
Published in Psychopharmacologia (01-04-1996)“…SR141716A (Sanofi Recherche), a pyrazole derivative with high affinity for rat and human CB1 cannabinoid receptors, has recently been reported to reverse…”
Get full text
Journal Article -
12
Characterization of Non-peptide Antagonist and Peptide Agonist Binding Sites of the NK1 Receptor with Fluorescent Ligands
Published in The Journal of biological chemistry (22-08-1997)“…Ligand recognition of the NK1 receptor (substance P receptor) by peptide agonist and non-peptide antagonist has been investigated and compared by the use of…”
Get full text
Journal Article -
13
3-Benzisothiazolylpiperazine Derivatives as Potential Atypical Antipsychotic Agents
Published in Journal of medicinal chemistry (05-01-1996)“…A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an…”
Get full text
Journal Article -
14
5-Phenyl-3-ureidobenzazepin-2-ones as cholecystokinin-B receptor antagonists
Published in Journal of medicinal chemistry (28-10-1994)“…A series of 5-phenyl-3-ureidobenzazepin-2-one cholecystokinin-B (CCK-B) receptor antagonists was synthesized using Beckmann ring expansion of a suitable…”
Get full text
Journal Article -
15
Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist
Published in Bioorganic & medicinal chemistry letters (03-02-1998)“…The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721,…”
Get full text
Journal Article -
16
A new class of selective and potent inhibitors of neuronal nitric oxide synthase
Published in Bioorganic & medicinal chemistry letters (06-09-1999)“…The synthesis and SAR of a series of 6-(4-(substituted)phenyl)-2-aminopyridines as inhibitors of nitric oxide synthase are described. Compound 3a from this…”
Get full text
Journal Article -
17
Nonpeptide tachykinin antagonists: medicinal chemistry and molecular biology
Published in Medicinal research reviews (01-11-1996)Get full text
Journal Article -
18
Antiinflammatory and analgesic activity of a non-peptide substance P receptor antagonist
Published in European journal of pharmacology (07-07-1992)“…CP-96,345, a potent non-peptide antagonist of the substance P (SP) receptor, inhibited SP-, neurokinin A (NKA)- and neurokinin B-induced plasma extravasation…”
Get more information
Journal Article -
19
Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase
Published in Journal of medicinal chemistry (01-02-1991)“…A series of quinazolinediones and azaquinazolinediones is described which possess potent inhibitory activity toward the calcium-independent phosphodiesterase…”
Get full text
Journal Article -
20
Tachykinin non-peptide antagonists: binding domain and molecular mode of action
Published in Biochemical Society transactions (01-02-1995)Get more information
Journal Article