The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The novel compounds provided by this invention have the Formula I: wherein R1 is H or methyl, R2 is H, azepanylcarbonyl, C1-C7 alkyl, —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo, R3 is C1-C5 alkyl, X is —NR4R5 or —OR7, R4 and R5 are independently H, C1-C5 alkyl, or R4 and R5 together with the nitrogen to which they are both bound form: R6 is —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo, A and B are independently —CO— or —CH2—, provided that A and B are not both —CO—, R7 is C1-C5 alkyl, Z is —CH2—, —O—, —S—, or —N(R8)—, R8 is H or C1-C6 alkyl, and n is 1 or 2.