Table 5

“Nonsedating” H1-receptor antagonists

AgentpKi valueReference
Temelastine9.5 Ter Laak et al. (1993)
Acrivastine9.2 Leurs et al. (1995b)
Epinastine8.9 Ter Laak et al. (1994)
Astemizole8.3 Ter Laak et al. (1993)
Cetirizine7.5 Ter Laak et al. (1993)
Terfenadine7.1 Ter Laak et al. (1993)
Loratidine6.8 Ter Laak et al. (1993)
  • Values are pKi (−log dissociation constant) determined from inhibition of [3H]mepyramine binding in homogenates of guinea pig cerebellum.