Aptiganel Hydrochloride

(USAN)

Chemical information

CNS-1102.
Chemical formula: C20H21N3,HCl = 339.9.
CAS — 137160-11-3.

Profile

Aptiganel is a guanidine derivative that antagonises the effects of the excitatory amino-acid neurotransmitter glutamate at NMDAreceptors. It has been investigated for the prevention of ischaemic brain damage in patients with traumatic head injury or stroke. A randomised controlled study4 in patients with acute ischaemic stroke was suspended because of a lack of efficacy and a potential imbalance in mortality compared with placebo.
1. Muir KW, et al. Pharmacological effects of the non-competitive NMDA antagonist CNS 1102 in normal volunteers. Br J Clin Pharmacol 1994; 38: 33–8
2. Block GA, et al. Final results from a dose-escalating safety and tolerance study of the non-competitive NMDA antagonist CNS1102 in patients with acute cerebral ischaemia. Stroke 1995; 26: 185
3. Dyker AG, et al. Safety and tolerability study of aptiganel hydrochloride in patients with an acute ischemic stroke. Stroke 1999; 30: 2038–42
4. Albers GW, et al. Aptiganel hydrochloride in acute ischemic stroke: a randomized controlled trial. JAMA 2001; 286: 2673–82.
Published December 24, 2018.