Table 2.

Summary of second-order rate constants for reaction of MTS compounds with receptors containing γ2D75C, γ2A79C, or γ2T81C in the absence (control) or presence of BZD ligands

ReceptorReagentControlFLZMRo 15–1788GABA
k2(m−1s−1)nk2(m−1s−1)nk2(m−1s−1)nk2(m−1s−1)n
αβγD75CMTSEA420  ± 2003530  ± 2103510  ± 2503580  ± 703
αβγA79CMTSEA-biotin1300  ± 2005670  ± 250*3600  ± 1002-16033700  ± 3002-1603
αβγT81CMTSEA-biotin-CAP17,000  ± 4400312,000  ± 170033700  ± 8002-160322,000  ± 23003
  • Second-order rate constants (k2) were derived by dividing the fit pseudo-first-order rate constants by the concentration of MTS reagent used (see Materials and Methods). The concentration of MTS compounds used was as follows (in μm): MTSEA, 200; MTSEA-biotin, 200; MTSEA-biotin-CAP, 20. Data represent mean ± SD values.

  • * ,

  • F2-160 Indicate values significantly different from control (MTS alone), with p < 0.05 andp < 0.01, respectively.