Odapipam is a benzazepine with high affinity and selectivity for D1-dopamine receptors. Labeled with C-11, it has been used as a PET radiotracer to visualize D1 receptors both in striatal and extrastriatal areas, such as the prefrontal cortex. Odapipam inhibits dopamine D1 receptor binding in vitro with low nanomolar to picomolar dissociation constants. The affinity of [11C]NNC 756 for D1 receptors is 0.18 nM. Odapipam was tested in phase I of clinical trials for the treatment of psychotic disorders, but failed.

Nolomirole (CHF1035) is an orally active, selective dopamine agonist, primarily activating DA2- and alpha2 receptors, thereby inhibiting norepinephrine release, which may be beneficial in heart failure. Nolomirole is able to attenuate the heart failure signs in the monocrotaline-induced congestive heart failure. CHF1035 is a mixture of two enantiomers, CHF1800 (+) and CHF1810 (-). CHF1035 and its metabolite CHF1024 significantly decreased the IOP in rabbits, and are potential novel IOP lowering agents. Especially, CHF1035 produced a substantial decrease in IOP for a prolonged period of time, and thus may prove useful in glaucoma therapy. Nolomirole is a pre-synaptic stimulator of DA2-dopaminergic and α2-adrenergic receptors in peripheral sympathetic nerve endings. These receptors act as a negative feedback mechanism, inhibiting norepinephrine secretion. In early phase clinical studies lasting 1–3 months, nolomirole reduced peripheral systemic resistance and 24 hour blood pressure and increased cardiac output. In a study of 29 patients with heart failure, followed for 10 days, a reduction in plasma norepinephrine was demonstrated. In spite of the fact that Nolomirole was in clinical trials for the treatment of heart failure, its development was discontinued.

Lirexapride serotonin 5-HT4 receptor and dopamine D2 receptor agonists. It had been in phase II clinical trials for the treatment of irritable bowel syndrome. However, this research has been discontinued.

Berupipam (also known as NNC 22-0010), a dopamine antagonist with a high affinity and selectivity for D1 receptor has been studied for patients with psychotic disorders. Berupipam participated in phase I clinical trials; however, further development of this drug was discontinued

Adoprazine (SVL-313) is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia and bipolar disorder. This drug together with some others, e.g. Mazapertine succinate, PF-217830 was discontinued from clinical trials due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy.

Butaclamol is an antipsychotic drug, which was studied for the treatment of schizophrenia. This drug has never marketed and now is used in research, because of its action as a dopamine receptor-blocking agent. Butaclamol consists of the two forms: (-)-butaclamol, an inactive drug and (+)-butaclamol, a potent neuroleptic drug.

Carvotroline [WY 47791] is a novel γ-carboline derivative with a preclinical profile suggestive of antipsychotic activity. Carvotroline has an affinity for the dopamine D2 receptor and cortical 5-HT2 receptor that is ten times greater than serotonin. Carvotroline administration to rats leads to a decrease of plasma corticosterone levels and demonstrated a moderating effect on the rotational-stress induced rise in plasma corticosterone levels.

The benzisoxazolyl piperidine derivative and atypical antipsychotic abaperidone [FI 8602] is being developed by Ferrer for the treatment of schizophrenia. Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.

Lensiprazine (SLV314) is a potent D2 receptor antagonist in vitro and have a considerable in vitro affinity for serotonin reuptake sites. It capable of antagonizing apomorphine-induced climbing behavior, disrupting CAR activity and potentiating 5-hydroxytryptophan (5-HTP) behavior. SLV314 has also been found to antagonize amphetamine- and ketamine-stimulated locomotor activity and methylphenidate-induced gnawing and stimulated behaviors, furthermore, a significant dose discrepancy was seen between the antipsychotic and cataleptogenic effects of SLV314. Lensiprazine demonstrated putative antipsychotic and selective serotonin reuptake inhibitor potential.