np-118809 and Pain

np-118809 has been researched along with Pain* in 1 studies

Other Studies

1 other study(ies) available for np-118809 and Pain

Article	Year
Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorganic & medicinal chemistry letters, 2009, Nov-15, Volume: 19, Issue:22 The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. Upon intraperitoneal administration both compounds exhibit analgesic activity in a rodent model of inflammatory pain. NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel. Topics: Analgesics; Animals; Binding Sites; Calcium Channel Blockers; Calcium Channels, L-Type; Calcium Channels, N-Type; Calcium Channels, T-Type; Disease Models, Animal; Drug Design; Pain; Pain Measurement; Pain Threshold; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship	2009

Article

Year

Scaffold-based design and synthesis of potent N-type calcium channel blockers.

Bioorganic & medicinal chemistry letters, 2009, Nov-15, Volume: 19, Issue:22

The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. Upon intraperitoneal administration both compounds exhibit analgesic activity in a rodent model of inflammatory pain. NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.

Topics: Analgesics; Animals; Binding Sites; Calcium Channel Blockers; Calcium Channels, L-Type; Calcium Channels, N-Type; Calcium Channels, T-Type; Disease Models, Animal; Drug Design; Pain; Pain Measurement; Pain Threshold; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2009