Nonpeptidic ligands for peptide and protein receptors

Distinct Mechanism for Antidepressant Activity by Blockade of Central Substance P Receptors

1998 • 1,067 citations

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

1998 • 455 citations

OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats.

1998 • 319 citations

Peptidomimetic design

1998 • 239 citations

Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist

1998 • 200 citations

Discovery of a Structurally Novel Opioid .KAPPA.-Agonist Derived from 4,5-Epoxymorphinan.

1998 • 176 citations

Potent, orally absorbed glucagon receptor antagonists

1999 • 168 citations

A Small, Nonpeptidyl Mimic of Granulocyte-Colony- Stimulating Factor

1998 • 153 citations

5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]- [1,4]benzodiazepin-10(11H)-ylcarbonyl)-3- chlorophenyl]benzamide (VPA-985): An Orally Active Arginine Vasopressin Antagonist with Selectivity for V₂Receptors

1998 • 144 citations

Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2

1998 • 128 citations

Discovery of a Novel, Potent, and Orally Active Nonpeptide Antagonist of the Human Luteinizing Hormone-Releasing Hormone (LHRH) Receptor

1998 • 126 citations

Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists

1998 • 122 citations

Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists

1999 • 90 citations

Novel Nonpeptide CCK-B Antagonists: Design and Development of Quinazolinone Derivatives as Potent, Selective, and Orally Active CCK-B Antagonists

1998 • 87 citations

A Novel Class of Orally Active Non-Peptide Bradykinin B₂ Receptor Antagonists. 3. Discovering Bioisosteres of the Imidazo[1,2-a]pyridine Moiety

1998 • 77 citations

Discovery of a Novel Non-Peptide Somatostatin Agonist with SST₄ Selectivity

1998 • 76 citations

Non-peptide ligands for peptide receptors

1989 • 74 citations

Peptidomimetic Growth Hormone Secretagogues. Design Considerations and Therapeutic Potential

1998 • 69 citations

De Novo Design, Synthesis, and Biological Activities of High-Affinity and Selective Non-Peptide Agonists of the δ-Opioid Receptor

1998 • 67 citations

Synthesis, Corticotropin-Releasing Factor Receptor Binding Affinity, and Pharmacokinetic Properties of Triazolo-, Imidazo-, and Pyrrolopyrimidines and -pyridines

1999 • 63 citations

2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N- methylamide (SDZ NKT 343), a Potent Human NK₁ Tachykinin Receptor Antagonist with Good Oral Analgesic Activity in Chronic Pain Models

1998 • 63 citations

Development of Orally Active Oxytocin Antagonists: Studies on 1-(1-{4-[1-(2-Methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl}piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and Related Pyridines

1998 • 62 citations

A Novel Class of Orally Active Non-Peptide Bradykinin B₂ Receptor Antagonists. 4. Discovery of Novel Frameworks Mimicking the Active Conformation

1998 • 59 citations

The design of non-peptide human bradykinin B2 receptor antagonists employing the benzodiazepine peptidomimetic scaffold

1999 • 57 citations

Identification of an Opioid κ Receptor Subtype-Selective N-Substituent for (+)-(3R,4R)-Dimethyl-4-(3-hydroxyphenyl)piperidine

1998 • 52 citations

PD 176252 — The first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist

1998 • 48 citations

A Potent, Orally Bioavailable Benzazepinone Growth Hormone Secretagogue

1998 • 44 citations

Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models

1998 • 43 citations

Second Generation “Peptoid” CCK-B Receptor Antagonists: Identification and Development ofN-(Adamantyloxycarbonyl)-α-methyl-(R)-tryptophan Derivative (CI-1015) with an Improved Pharmacokinetic Profile

1998 • 43 citations

Biphenylsulfonamide Endothelin Antagonists: Structure−Activity Relationships of a Series of Mono- and Disubstituted Analogues and Pharmacology of the Orally Active Endothelin Antagonist 2‘-Amino-N- (3,4-dimethyl-5-isoxazolyl)-4‘-(2-methylpropyl)[1,1‘-biphenyl]-2-sulfonamide (BMS-187308)

1998 • 39 citations

A Novel Class of Orally Active Non-Peptide Bradykinin B₂ Receptor Antagonists. 2. Overcoming the Species Difference between Guinea Pig and Man

1998 • 38 citations

Pharmacological characterization of a nonpeptide bradykinin B₂ receptor antagonist, FR165649, and agonist, FR190997

1998 • 35 citations

1-[2(R)-(2-Amino-2-methylpropionylamino)-3-(1H-indol-3-yl)propionyl]-3- benzylpiperidine-3(S)-carboxylic Acid Ethyl Ester (L-163,540): A Potent, Orally Bioavailable, and Short-Duration Growth Hormone Secretagogue

1998 • 35 citations

Novel Orally Active Growth Hormone Secretagogues

1998 • 34 citations

Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist

1998 • 33 citations

High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template

1998 • 29 citations

4,4-Disubstituted Piperidine High-Affinity NK₁ Antagonists: Structure−Activity Relationships and in Vivo Activity

1998 • 28 citations

Pyrrolidine-3-carboxylic Acids as Endothelin Antagonists. 3. Discovery of a Potent, 2-Nonaryl, Highly Selective ET_A Antagonist (A-216546)

1998 • 23 citations

Potent, orally bioavailable somatostatin agonists: Good absorption achieved by urea backbone cyclization

1999 • 21 citations

Selective Endothelin A Receptor Antagonists. 3. Discovery and Structure−Activity Relationships of a Series of 4-Phenoxybutanoic Acid Derivatives

1998 • 19 citations

Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptor-ligand interactions

1998 • 17 citations

Motilides and motilactides: Design and development of motilin receptor agonists as a new class of gastrointestinal prokinetic drugs

1998 • 15 citations

Update on nonpeptide CCK-B receptor antagonists

1998 • 15 citations

3. Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist

1998 • 14 citations

Synthesis of 9-Deoxo-4‘‘-deoxy-6,9-epoxyerythromycin Derivatives: Novel and Acid-Stable Motilides

1998 • 13 citations

Synthesis of Phenoxyacetic Acid Derivatives as Highly Potent Antagonists of Gastrin/Cholecystokinin-B Receptors. II.

1998 • 11 citations

L-tryptophan urea amides as dual antagonists

1998 • 11 citations

Thieno[2,3-d]pyrimidine-3-acetic Acids A New Class of Nonpeptide Endothelin Receptor Antagonists.

1998 • 10 citations

4-Alkylpiperidines related to SR-48968: Potent antagonists of the neurokinin-2 (NK2) receptor

1998 • 9 citations

Studies on Nonpeptide Angiotensin II Receptor Antagonists. II. Synthesis and Biological Evaluation of 5H-Pyrazolo(1,5-b)(1,2,4)triazole Derivatives with a C-Linked Oxygen Functional Group at the 6-Position.

1998 • 7 citations

Stereoselective synthesis of a novel and bifunctional endothelin antagonist, IRL 3630

1998 • 7 citations