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

T Harrison; M P Korsgaard; C J Swain; M A Cascieri; S Sadowski; G R Seabrook

doi:10.1016/s0960-894x(98)00215-7

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

Bioorg Med Chem Lett. 1998 Jun 2;8(11):1343-8. doi: 10.1016/s0960-894x(98)00215-7.

Authors

T Harrison¹, M P Korsgaard, C J Swain, M A Cascieri, S Sadowski, G R Seabrook

Affiliation

¹ Department of Medicinal Chemistry, Merck Sharp Laboratory, Essex, U.K. timothy_harrison@merck.com

PMID: 9871763
DOI: 10.1016/s0960-894x(98)00215-7

Abstract

High affinity, selective hNK2 or hNK3 ligands can be prepared from the common template 1 in a few simple chemical operations. The hNK3 ligands 3 antagonise the calcium mobilisation caused by activation of hNK3 receptors expressed in CHO cells as measured using fura-2 microspectrofluorimetry.

MeSH terms

Animals
CHO Cells
Calcium / metabolism
Cricetinae
Fluorescent Dyes
Fura-2
Humans
Lactams / chemical synthesis*
Lactams / pharmacology
Molecular Conformation
Receptors, Neurokinin-2 / antagonists & inhibitors*
Receptors, Neurokinin-2 / chemistry
Receptors, Neurokinin-3 / antagonists & inhibitors*
Receptors, Neurokinin-3 / chemistry
Spectrometry, Fluorescence
Structure-Activity Relationship

Substances

Fluorescent Dyes
Lactams
Receptors, Neurokinin-2
Receptors, Neurokinin-3
Calcium
Fura-2