2. GPCR/G Protein
  3. CaSR
  4. NPS-467

NPS-467 is a calcium-sensing receptor (CaR) activator and stereospecific agent with only its R-enantiomer active. NPS-467 increases the sensitivity of the CaR to activation by extracellular calcium. NPS-467 stimulates stanniocalcin (STC) secretion in trout and induces inhibition of gill calcium transport in trout. NPS-467 has no effect on serum calcitonin levels in trout.

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NPS-467

NPS-467 Chemical Structure

CAS No. : 148717-47-9

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Description

NPS-467 is a calcium-sensing receptor (CaR) activator and stereospecific agent with only its R-enantiomer active. NPS-467 increases the sensitivity of the CaR to activation by extracellular calcium. NPS-467 stimulates stanniocalcin (STC) secretion in trout and induces inhibition of gill calcium transport in trout. NPS-467 has no effect on serum calcitonin levels in trout[1].

In Vivo

NPS-467 (R-enantiomer) (0.25-8.0 mg/kg; i.p.; single dose) produces stereospecific, dose- and time-dependent stimulation of STC secretion in juvenile rainbow trout, with an ED50 of 0.44 mg/kg and a maximal 9-fold increase in serum STC levels, while having no effect on serum CT levels[1].
NPS-467 (R-enantiomer) (0.25-2.0 mg/kg; i.p.; single dose) produces stereospecific, dose-dependent inhibition of gill calcium transport in fingerling rainbow trout via enhanced STC release, with an ED50 of 0.5 mg/kg, and this effect is fully blocked by fish STC antiserum[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Oncorhynchus mykiss (juvenile, 150-250 g)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
Administration: i.p.; single dose
Result: Produced statistically significant stimulatory effects on STC secretion (P < 0.01-0.001).
Raised serum STC levels maximally to 2069 ng/mL, representing a 9-fold induction over controls; the response plateaued at doses above 2.5 mg/kg.
Achieved an ED50 of 0.44 mg/kg for STC secretion stimulation.
Induced a rapid response, with maximal 14-fold STC induction by 0.5 hours post-injection, which persisted for up to 4 hours.
Showed no statistically significant effects on serum CT levels at doses of 0.25, 0.5, 1.0, or 2.0 mg/kg.
Animal Model: Oncorhynchus mykiss (fingerling, 1-2 g)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
Administration: i.p.; single dose
Result: Produced consistent, dose-dependent inhibitory effects on GCAT across three experiments, with statistically significant reductions at all tested doses (P < 0.05-0.01).
Achieved an ED50 of 0.5 mg/kg (2.5 μmol/kg) for GCAT inhibition, which was similar to the ED50 for STC secretion stimulation.
Had its inhibitory effects on GCAT at 2.0 mg/kg completely neutralized by passive immunization with fish STC antiserum, with GCAT rates not significantly different from controls receiving nonimmune rabbit serum alone.
Molecular Weight

269.38

Formula

C18H23NO
CAS No.
SMILES

CC(NCCCC1=CC=CC=C1)C2=CC(OC)=CC=C2
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References
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  • Do most proteins show cross-species activity?

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Keywords:

NPS-467148717-47-9NPS467NPS 467CaSRCalcium-sensing receptorcalcium-sensing receptorjuvenile rainbow troutserum calcitoninstanniocalcintroutgill calcium transportextracellular calciumfingerling rainbow troutCaRSTCInhibitorinhibitorinhibit

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