TABLE 2

EC50 and Ki values of nicotinic acid and related compounds

CompoundRataHumanb
GTPγS Binding Assay (EC50)[3H]Nicotinic Acid Binding Assay (Ki)GTPγS Binding Assay (EC50)[3H]Nicotinic Acid Binding Assay (Ki)
AdipocytesSpleenSpleenHCA2 (Cloned)HCA2 (Cloned)Adipocytes
μM
Nicotinic acid1.40.700.0330.250.0810.079
AcifranN.D.N.D.N.D.2.11.10.83
Acipimox106.60.316.05.14.3
3-Pyridine-acetic acid16170.405.50.540.55
Pyridazine-4-COOH3.83.10.12N.D.N.D.N.D.
Pyrazine-2-COOH26220.76N.D.N.D.N.D.
5-Me-nicotinic acid30300.728.74.123.68
5-Me-pyrazine-2-COOH52150.65N.D.N.D.N.D.
6-Me-nicotinic acid73541.7N.D.N.D.N.D.
Nicotinic acid-1-oxide80743.2N.D.N.D.N.D.
2-OH-nicotinic acid132N.D.N.D.N.D.N.D.N.D.
Furan-3-COOH142N.D.N.D.N.D.N.D.N.D.
Nicotinamide>1000>1000N.D.>10009275
  • N.D., not determined.

  • a Lorenzen et al. (2001).

  • b Wise et al. (2003).