FEATURES

FAMILY

DESCRIPTION

Also known as CRF1_CONCF, CRF1. Conorfamide As1a: this amidated form is active on both ASIC channels and nicotinic acetylcholine receptors (nAChRs) (PubMed:31028742). Shows a weak inhibition of peak current of rat ASIC1a and rat ASIC3 (PubMed:31028742). Inhibits desensitization of ASIC1a and to a lesser degree ASIC3 currents, resulting in a sustained opening of channels in the presence of low pH (PubMed:31028742). Inhibits with a slow reversibility human alpha-7/CHRNA7 nAChRs (IC(50)=737-4984 nM) and with rapid reversibility human alpha-1-beta-1-delta-epsilon (CHRNA1-CHRNB1-CHRND-CHRNE) nAChRs (IC(50)=215 nM) (PubMed:31028742)., Conorfamide As1b: this non-amidated form is only weakly active on both ASIC channels and nicotinic acetylcholine receptors (nAChRs) (PubMed:31028742). Shows a weak inhibition of peak current of rat ASIC1a (PubMed:31028742). Shows a very weak inhibition of peak current of rat ASIC3 (PubMed:31028742). No inhibition of desensitization on both rat ASIC1a and ASIC3 are observed (PubMed:31028742). Reversibly inhibits both human alpha-7/CHRNA7 nAChRs (IC(50)=2029-8464 nM) and human alpha-1-beta-1-delta-epsilon (CHRNA1-CHRNB1-CHRND-CHRNE) nAChRs (IC(50)=820 nM) (PubMed:31028742).

CRF1

Structural Ligandability

Domains Chains

Distribution