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  1. Rotigotine is used to treat Parkinson's disease. Rotigotine acts as a non-selective agonist of the dopamine D1, D2, D3, and, to a lesser extent, D4 and D5 receptors, with highest affinity for the D3 receptor.[10] In terms of affinity, rotigotine has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor.[10] In functional studies however, rotigotine behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50). Receptor Binding Profile of Rotigotine: D1 receptor (Ki = 83 nM) D2 receptor (Ki = 13.5 nM) D3 receptor (Ki = 0.71 nM) D4.2 receptor (Ki = 3.9 nM) D4.4 receptor (Ki = 15 nM) D4.7 receptor (Ki = 5.9 nM) D5 receptor (Ki = 5.4 nM) Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well.[3]
  2. The following drugs act as dopamine receptor D1 agonists. Theoretically, this effect can be useful in treating negative symptoms of schizophrenia: which are hypothesized to be due to hypoactivity of D1 receptors. Stepholidine is a D1 agonist and D2 antagonist showing antipsychotic effects.Dinapsoline is a potent selective full agonist at D1 receptors. Used for Parkinson's disease.Dinoxyline is a potent full agonist at all five dopamine receptors: D1, D2, D3, D4, and D5. Dihydrexidine is a moderately selective full agonist at the D1 & D5 receptors. It has a 10-fold selectivity for D1 & D5 over D2.Pergolide is a weak D1 agonist and highly selective D2 agonist. It is also agonist on several serotonin receptors just like Bromocriptine.
  3. RopiniroleRopinirole is a D2, D3, and D4 dopamine receptor agonist. Its affinity for D3 receptors is 20 times greater than for D2 receptors [1]. Ropinirole is useful in treating SSRI-induced sexual dysfunction [2]. Ropinirole could be useful as an adjunctive treatment for treatment-resistant depression [3] Ropinirole is also useful in treating negative symptoms of schizophrenia [4]. Ropinirole is primarily used in the treatment of Parkinson's disease.PramipexolePramipexole is also primarily used in the treatment of Parkinson's disease. Pramipexole is also a D2-like receptor agonist: D2, D3, and D4, with the following intrinsic activities:D2L [70%] = high partial agonistD2S [130%] = superagonistD3 [70%] = high partial agonistD4 [42%] = partial agonistPramipexole has highest affinity for D3 receptors. Pramipexole is also useful as an adjunctive treatment for depression, anhedonia [5], and negative symptoms.CabergolineCabergoline is a D1, D2, D3, and D4 agonist. Cabergoline also has agonistic activity on 5HT1A and 5HT2A receptors. It is used to lower prolactin levels and treat SSRI-induced sexual dysfunction (low libido, anorgasmia) [6]. It can be used as an aphrodisiac, as it boosts libido, intensifies orgasms, and enhances sexual performance (shortens the refractory period after an orgasm) [7], that is, with Cabergoline people can skip the post orgasm hangover. BromocriptineBromocriptine is a potent agonist at dopamine D2 receptors and various serotonin receptors. It also inhibits the release of glutamate. Bromocriptine is used to treat hyperprolactinaemia (high prolactin levels), neuroleptic malignant syndrome, and Parkinson's disease [1]. Bromocriptine is also used to treat infertility, hypogonadism and diabetes II [1]. Bromocriptine has also been found to reduce negative symptoms of schizophrenia [2].Pharmacodynamics of Bromocriptine - Receptor Binding Profile: Dopamine D1 family D1 (Ki=682 nM) D5 (Ki=496 nM) Dopamine D2 family D2 (Ki=2.96 nM) D3 (Ki=5.42 nM) D4 (Ki=328 nM) Serotonin 5-HT 5-HT1A (Ki=12.9 nM) 5-HT1B (Ki=355 nM) 5-HT1D (Ki=10.7 nM) 5-HT2A (Ki=107 nM) 5-HT2B (Ki=56.2 nM) 5-HT2C (Ki=741 nM) 5-HT6 (Ki=33 nM) Note: Ki = dissociation constant. The smaller the Ki value, the stronger the affinity (chemical binding strength).
  4. Welbutrin (Bupropion) is a dopamine-norepinephrine reuptake inhibitor; its occupancy at dopamine transporter (DAT) is 23%; whereas over 75% causes euphoria (ex. cocaine). A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. I am currently taking Abilify 400 mg every 3 weeks (~ 20 mg / day) and 300 mg of Welbutrin. I was complaining to my psychiatrist about the side effects of Abilify I was suffering from; depression (low mood), sexual dysfunction, anhedonia, from a condition called "Neuroleptic Induced Deficit Syndrome" . I complained that I had totally lost my motivation, drive, and initiative and was experiencing anhedonia (lack of pleasure), emotional suppression, etc. It is like living in a mental restraint "straigthjacket". So my psychiatrist added Welbutrin. Abilify dampens down dopaminergic activity in three of the four dopaminergic pathways; It is the only Antipsychotic that I know of that can increase mesocortical dopaminergic activity. Other partial agonists like Brexiprazole and Cariprazine might do this also, whereas a silent antagonist cannot. Welbutrin has treated my low mood; I am euthymic now, but I am still anhedonic from Abilify being so frequent for such a dose; I am taking the daily equivalent of 20 mg: 400 mg per 3 weeks. At lower doses Abilify has a more stimulating effect. The Welbutrin he added certainly helps; but is unfortunately not enough. I am considering adding a dopamine full agonist such as Ropinirole, Rotigotine, Cabergoline and Pramipexole to my prescription meds. Some dopamine agonists are useful at treating depression resistant to SSRI-treatment. Dopamine agonists can be given to counteract the side effects of antipsychotics and serotonergic antidepressants. No doubt that dopamine antagonism has a negative effect on mood. In the mesolimbic pathway *(reward pathway)* Aripriprazole reduces dopaminergic activity; which reduces motivation - salience (liking, rewarding), which can be identified as a major source of anhedonia. Aripriprazole does not reduce dopamine transmission in the mesocortical pathway in people whose mesocortical pathway has .less than normal activity. The dopamine boost that Welbutrin provides keeps me stable; counterbalances some of the negative effects of Abilify. I just need more help in alleviating this zombified state of existence in which I am alienated from my own real self. and cannot enjoy the things I used to enjoy; food, drugs, sex. I live in anhedonia, a state of a loss of pleasure; due to the neurological inhibition caused by Abilify. Welbutrin works as a wakefullness promoting agent, a mild stimulant.
  5. Aripriprazole is a dopamine D2 partial agonist (30%) on posynaptic receptors and partial agonist (75%) on presynaptic receptors . At low doses it has an stimulating effect. At high doses it has a sedative effect. Aripriprazole is a 5HT1A partial agonist (68%) also; which leads to dopamine release in the prefrontal cortex. Due to partial agonism on D2, D3, D4, Aripriprazole modulates dopamine levels in the mesocortical pathway; by increasing activity where it is absent or low; and reducing activity where it is high. Aripriprazole is also a 5HT2A antagonist as are atypical antipsychotics; this has antipsychotic and anti-manic effects. Look out for dopamine supersensitivity; The long term use of antipsychotics causes extra dopamine receptors to be produced by the brain; this is called upregulation. The brain's dopamine receptors upregulate under the blockade of the antipsychotic agent. Antipsychotics cover 70% - 90% of dopamine receptors. The brain, in an effort to maintain homeostatic equilibrium produces more dopamine receptors on receiving neurons in order to sensitize the neurons to dopamine called "dopamine supersensitivity" which is associated with a risk of relapse. Antipsychotics have withdrawal effects; So taper off the antipsychotic; do not abruptly withdraw the drug.
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