dopamine D2 receptors: nootropics and compounds | sci-wiki

Aripiprazole

Aripiprazole is a second-generation (atypical) antipsychotic used in schizophrenia, bipolar disorder and as an adjunct in major depression. Rather than fully blocking dopamine D2 receptors like older agents, it acts as a high-affinity partial agonist, combined with partial agonism at serotonin 5-HT1A and antagonism at 5-HT2A receptors, so that it behaves as a dopamine system stabilizer that dampens signaling where dopamine is excessive and supports it where dopamine is deficient. This mechanism gives it antipsychotic efficacy comparable to other agents with relatively little sedation, weight gain, movement disorder or prolactin elevation, and it is also formulated as a long-acting monthly injection to support adherence. The same partial-agonist pharmacology, however, can occasionally provoke impulse-control problems such as pathological gambling, an effect it shares with dopamine agonists.

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Dopaminergic

Bromocriptine

Bromocriptine is a dopamine receptor agonist derived from ergot, acting mainly at the dopamine D2 receptor. It is used to treat conditions linked to excess prolactin, such as prolactinomas and related infertility, as well as Parkinson disease, acromegaly, and, in a quick-release form, type 2 diabetes. Discovered by Sandoz in the 1960s, it was approved for medical use in the 1970s.

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Dopaminergic

Cabergoline

Cabergoline is a long-acting, ergot-derived dopamine agonist that acts mainly at the dopamine D2 receptor. It is used chiefly to treat conditions of excess prolactin, especially prolactin-secreting pituitary tumors (prolactinomas), and is also used in Parkinson disease and acromegaly. Because of its long duration of action it is usually taken only once or twice a week.

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Antipsychotic

Olanzapine

Olanzapine is an atypical, or second-generation, antipsychotic used to treat schizophrenia and bipolar disorder. Chemically a thienobenzodiazepine, it was discovered in a search for compounds resembling clozapine but without that drug's blood-monitoring requirement, and it works by blocking a broad range of dopamine and serotonin receptors. Beyond psychiatry it is a highly effective antiemetic and appetite stimulant even at very low doses, which is used in cancer care, though it is among the antipsychotics most likely to cause weight gain and metabolic problems, prompting the development of an olanzapine-samidorphan combination to blunt that effect.

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Antipsychotic

Quetiapine

Quetiapine is an atypical, or second-generation, antipsychotic used to treat schizophrenia, bipolar disorder, and, as an add-on, major depression. Its effects are strongly shaped by dose and by its active metabolite norquetiapine, which inhibits the norepinephrine transporter and modulates several serotonin receptors, giving quetiapine genuine antidepressant activity; at low doses its dominant action is sedating H1-antihistamine blockade with little dopamine occupancy, while antipsychotic dopamine blockade emerges only at higher doses. Marketed originally as Seroquel and now generic, it is on the World Health Organization list of essential medicines and is also widely, though generally discouraged, prescribed off-label as a sedative for insomnia.

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Blend

Rabeprazole + Domperidone

Rabeprazole plus domperidone is a fixed-dose combination medicine that pairs two drugs acting on the upper digestive tract: rabeprazole, a proton pump inhibitor that suppresses stomach acid, and domperidone, a prokinetic and antiemetic that speeds the movement of food out of the stomach. The combination is used mainly for acid reflux and related conditions accompanied by nausea, bloating, or slow gastric emptying. It is marketed in India and various other countries, often as a single capsule, but it is not approved in the United States, where domperidone itself is unlicensed.

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