Recent advances in central dihydropyridine (DHP)-binding sites are reviewed. DHP-binding sites are pre-synaptically and post-synaptically localized in the brain. The functional role of post-synaptic sites is still unknown, whereas pre-synaptic sites seem to contribute to the control of calcium uptake and of neurotransmitter release. DHP-binding sites may be modualated in physiological (age, sex) and pathological events (hypertension, ischaemia, neurological diseases) or after drug treatments (alcohol, morphine, etc.). The reviewed data suggest new therapeutic implications of DHP calcium channel antagonists in the treatment of other diseases and of drug withdrawal syndrome.