Table 1.
Orthosteric agonists and allosteric modulators of the calcium-sensing receptor (modified from [110]).
| Orthosteric Agonists (Type I Calcimimetics) | Class Members |
| A. Cations | High potency: Gd3+; Eu3+; Tb3+ |
| Intermediate potency: Zn2+; Ni2+; Cd2+; Pb2+; Co2+; Fe2+ | |
| Low potency: Ca2+; Mg2+; Ba2+; Sr2+; Mn2+ | |
| B. Polyamines | spermine, spermidine, putrescine |
| C. Aminoglycoside antibiotics | neomycin, gentamycin, tobramycin, poromomycin, kanamycin, ribostamycin |
| D. Basic polypeptides | Poly-L-arginine, poly-L-lysine, protamine, amyloid β-peptides |
| Allosteric Modulators (Type II Calcimimetics) | |
| A. L-amino acids | phenylalanine, tryptophan, tyrosine, histidine |
| B. Glutathione analogs | γ-glutamyl-tripeptides: glutathione, S-methylglutathione, S-propylglutathione, γ-glutamyl-tripeptides (γ-Glu-Ala, γ-Glu-Cys) |
| C. Small molecule calcimimetics | The first generation: NPS R-568, NPS R-467, AMG 073, AMG 416 |
| The second generation: cinacalcet | |
| The third generation: dibenzylamine calcimimetics, R,R-calcimimetic B, AC-265347 | |
| D. Small molecule calcilytics | NPS 2143, Calhex 231, ATF396, AXT914, ronacaleret, NPSP795, SB-423557, SB-423562 |