what receptors do the antidepressants and antianxiety medications act on?

what is receptors function database:

info about what reaction will happen if you agonist/antagonist the receptors,

keep in your mind, the place of the receptor can make change of the receptor function, like agonizing adrenergic β2 receptor in the heart will cause fast heart beat and hypertension, but agonizing them in the brain will cause urge to fight, by increasing reward for violence behaviors..

add to that this is just self gathering info for multiple source, as of what i understand in the over last years of testing, my info might be wrong, it's just will help you to know more about the general function of the receptor, thanks ☺

advantages:

-to cell are colored for knowing its better to agonist the receptor or antagonist it

-link for source are available (to read where i got this info, available only in excel file down, not image or html type)

-endogenous and exogenous affinity to the receptors are available

-always updated info because i never got boring from exploring ☺✌

-free

preview:

green: in (whats will happen if) cell mean = I am not sure if the information is correct in that cell
in (receptor) cell mean = transporter.

blue: in (whats will happen if) cell mean = I'm sure.
in (receptor) cell mean = better to agonist.

red:in (receptor) cell mean = better to be antagonist.

  black blue: in (receptor) cell mean = agonizing give strong benefits

   black red: in (receptor) cell mean = antagonizing give strong benefits

yellow: just additional info

auto-receptor: the receptor that product negative feedback mean it will decrease the release of it's endogenous neurotransmitter

anti-target: pharmacy companies (eg, Eli Lilly) always make sure their drugs doesn't interact with that receptor because it cause problems

 

html table:

Neurotransmitters

selectivity (Ki nm)

receptor

what's will happened if

endogenous

exogenous

agonized/enhanced

antagonized/inhibited

serotonin

/

SERT

Serotonin reduction

increase serotonin

decrease D2 sensivity in striatal

downregulate dopamine 3 receptors

1.0

HT1A

feelings of love, empathy, and connection to others by induceding oxytocin stimulation

negative feedback

Antidepressants (post-synaptic receptor agonists and pre-synaptic autoreceptor antagonists serve as antidepressants

depressant

1.4

HT1B

induced repetitive behavior  of ocd

negative feedback

aggression

anxiolytic

implusivity (by increasing dopamine levels and dopamine release in the nucleus accumbens the place most expressed D3 receptors)

1.6

HT1D

negative feedback

Vasoconstriction

inhibit/modulating release of glutamate

antidepressant

affects locomotion and anxiety

2.4

HT1E

might involved in the regulation of memory in humans

2.6

HT7

Autoreceptor

antidepressant & Cognition & ability to regonise old objects

2.6

HT2C

increase of corticotropin releasing hormone (CRH) and vasopressin mRNA in the paraventricular nucleus and proopiomelanocortin in the anterior pituitary lobe. In rats

decrease impulsivity and motivation for drug and food

reduced cognitive deficits

anxiolytic or sometimes in some aspect anxiety

estradiol and progesterone decrease the receptor concentration in the ventral hippocampus

increases release serotonin,  norepinephrine and dopamine

2.8

HT2B

empathy

Autoreceptor

Required for behavioral effects of SSRIs

pulmonary hypertension

3.2

HT1F

treatment of migraine headaches

development was halted due to toxicity

3.6

HT2A

hallucination

anti-inflammatory

inhibit dopamine release and increases in hormonal levels of oxytocin, prolactin, ACTH, corticosterone, and renin

antidepressant

Serotonin syndrome

antidepressant

31.0

HT6

anti-anxiety

antidepressant

increase GABA

Antagonists enhance cognitive performance; blockade of signaling is anxiogenic

reverse a scopolamine-induced cognitive deficit but it appears that 5-HT6 receptor blockade is more consistently effective in alleviating memory deficits than increasing memory in normally functioning animals

Alzheimer's disease

block effect of ssris

39.7

HT4

Ememory & learning + antidepressant effects

increase acetylcholine

respiratory depression

79.2

HT5A

Autoreceptor + Memory consolidation

implicated in the sleep-wake cycle

187.1

HT3

Serotonin syndrome

Anti-vomiting

anxiolysis

antidepressant

dopamine

/

DAT

dopamine reduction

increase dopamine

1.0

D1

in prefrontal cortex : cognition-enhancing effects

hypotension

D1 receptors in the 'direct pathway' provide a range of possible decisions derived from activity in the cortex

rewarded behaviors and pleasure, One such behavior is eating + nootropic, anorectic, rewarding and profound antiparkinson effects

motivation (goal directed behaviors)

anxiety and depression

effective antagonist d1(mostly the cause)/d5 product inhibition of acute euphoric effects of cocaine

treatment of Tourette's syndrome

1.0

D2

D2 receptors in the 'indirect pathway' are activated to filter and select one of decisions provided by D1 receptor, add to that increase reward for complex stuff like:  internet, big dreams , urge/enjoyment to Efficiency complete tasks (over activation if together with anxiety cause ocd) etc..

hyperactivity of adhd

induce locomotion activity

reduce prolactin

Anti-vomiting

Neuroleptic malignant syndrome

antipsychotic positive symptoms

extrapyramidal symptoms  especially  dystonia

D2s

negative feedback: reduce dopamine release and increase dopamine reuptake

1.0

D3

increase reward for: shopping, gambling, eating, sex, drug seeking behaviors', Risk-Taking , impulsivity

Stimulation of yawning

anti-empathy effect

anti-restless leg syndrome

reduce prolactin

Anti-vomiting

block agitation induced by of D3 agonizing

Blockade of the D3 receptor disrupts drug-associated cue-induced craving and stress-induced craving.

fear from risk-taking stations

induce sexual fantasies

poriomania (A morbid impulse to wander or journey away from home.)

kleptomania (a recurrent urge to steal, typically without regard for need or profit.)

Intermittent explosive disorder or IED is a clinical condition of experiencing recurrent aggressive episodes that are out of proportion of any given stressor.

Pyromania: is characterized by impulsive and repetitive urges to deliberately start fires.

1.0

D4

Novelty seeking (increases the propensity for exploring to select a novel choice over familiar one (eg, human example in this is relationship cheating))

increase working memory performance and fear

reverse stress-induced working memory deficits

associated with cheating, like in sex relationships and might other type of cheating too..

D4.7

better cognitive performance

x10 of D1

D5

inhibits the synthesis of melatonin

reduces burst firing  and improve motor deficits, increased motor response to administration of methamphetamine

learning problems (fear memory aid by B2 and M1 receptors) that may be associated with ADHD

hypertension

noradrenalin

/

NET

nordraline reduction

increase nordraline

/

α1

vasoconstriction

anorexia

inhibit hearing system

orthostatic hypotension

inhibit ejaculation but not orgasm

1.2

α1A

inhibit olfactory system

1.0

α1B

no info in Wikipedia

/

α1C

1.6

α1D

/

α2

vasoconstriction

anti ptsd + anxiety disorders

1.5

α2A

in prefrontal cortex : cognition-enhancing effects + lowering blood pressure

negative feedback: at high stimulation frequencies

1.4

α2B

emotional memory focus more on negative aspects of a situation

1.5

α2C

negative feedback : at lower levels of nerve activity

1.3

β1

anxiolytic

in (SNS) positive feedback

lower blood pressure

bronchoconstriction (less affective then β2)

1.1

β2

increase rewards for: fighting, listening rap music, social dominance

nervous and excitable, increase respiration speed, fine visual Hallucinations, rather not to say empathy talk

bronchoconstriction

1.1

β3

induce fat breaking in adipose tissue / anti muscle stress effects

antidepressant and anxiolytic

tremors

histamine

102.9

H1

orthostatic hypotension

Sleep-wake cycle (promotes wakefulness), body temperature, nociception, endocrine homeostasis, regulates appetite, involved in cognition

anti-sensitivity

anti-insomnia

anti-acne

dizziness

15.8

H2

The ulcer

6.8

H3

autoreceptors

anti-vertigo

increase histamine, acetylcholine, norepinephrine, serotonin, GABA release

stimulant + wakefulness + cognitive enhancing at relatively low levels of receptor occupancy

improve memory consolidation

17.1

H4

anti-inflammatory and antihyperalgesic effects

acetylcholine

asyt T

increase acetylcholine

1.0

M1

Secretion from salivary glands

aggression

Secretion from salivary glands

Gastric acid secretion from stomach and muscle spasm.

olfactory behaviors (e.g. mating is the pairing of either opposite-sex or hermaphroditic organisms )

inhibit ability of recall memory

Delirium hallucinations

100.9

M2

negative feedback

slow the heart rate

Responsible for decrease in sexual activity, as a study using rats confirmed

Mediating olfactory guided behaviors (e.g. odor discrimination, aggression, mating).[10]

235.3

M5

Stimulation of gastric acid secretion.

increase dopamine release

M5 receptor knockout mice exhibit a reduction in the reinforcing effects and withdrawal symptoms of cocaine and morphine

M4

hypersalivation

inhibit D1-induced locomotion stimulation

Inhibition of dopaminergic (D1 receptor) signaling

negative feedback

treatment of Parkinson's disease

knockout mice exhibit an increase in anxiolysis compared to wild-type mice

M3

increased secretions from stomach (emesis)

change glucose to weight gain (olanzpine)+diabetes side-effects

decreases the urgency to urinate

anti-asthma

nicotine

α1

no info in the first 100 Google search result

α2

influence hippocampus-dependent learning and memory and behaviors

α3

Heterozygous α3 mice are less sensitive to nicotine-induced seizures.

α4

induced release of dopamine

more sensitive to nicotine-induced hypothermia and nicotine-induced seizures and sleep disruptions

altered nicotinic modulation of respiratory rhythm

α5

Knockout mice show increased nicotine intake in self-administration tests, Reduced sensitivity to nicotine-induced behavioral effects and seizures, Increased attentional performance

22.35

7,75 (nicotine)

α6

increase reward and reinforcing effects

103,14 (nicotine)

α7

some of the cognitive effects of nicotine

α8

no info in the first 100 Google search result

α9

α10

no info in the first 100 Google search result

β1

expressed in vertebrate skeletal muscle and placenta

β2

increase attentional performance

Knockout mice loss of nicotine-induced dopamine and GABA release, impaired development of the visual system, increased passive avoidance latency; loss of nicotine self-administration, reduced nicotine-induced antinociception, impaired learning and increased neurodegeneration in aged animals

β3

chronic exposure induced withdrawal

Modulation of gene expression and increase nicotine consumption

Modulate Dopamine Release

hyperalgesia, anhedonia-like effect

β4

Knockout mice display decreased anxiety-related responses; resistance to nicotine-induced seizures; decreased nicotine withdrawal

Nicotine intravenous self-administration (IVSA) was lower in constitutive β4 knockout (KO) mice at all doses tested, β4KO mice have higher extracellular dopamine (DA) levels in the nucleus accumbens

γ

expressed in adult extraocular muscle and involvement in myasthenia gravis

δ

no info in the first 100 Google search result

ε

knockout mice display impaired neuromuscular transmission, progressive muscle weakness and atrophy and associated with the human AChR deficiency syndrome

3.04

1 (nicotine)

α4β2

improvements in attentional performance

release of dopamine in the nucleus accumbens

2.24

1,38 (nicotine)

α2β2

16.47

3,48 (nicotine)

α3β2

23.09

8,68 (nicotine)

α4β4

32.35

23,57 (nicotine)

α2β4

21.18

37,98 (nicotine)

α6β4

36.18

50,78 (nicotine)

α6β2

60,47 (nicotine)

α6β3β4α5

230.29

92,95 (nicotine)

α3β4

anti-addiction

Sigma

σ1

hallucinogenic

nootropic and antidepressant actions in animal studies, as well as antitussive

anti-amnesic

antipsychotic

decreases the convulsivity

σ2

no role in depression

regulate cholesterol transporter NPC1, involved in cholesterol homeostasis

glutamate transporter

EAAT2

induce/enhance the expression of EAAT2=reduce the development and expression of tolerance to opiates and other drugs of abuse

reduced expression of EAAT2= increase addictive/drug-seeking behavior and increase in vulnerability to relapse after re-exposure to the addictive drug or its associated drug cues

NMDA

GluN1 (glycine)

plasticity of synapses which is believed to underlie memory and learning

anxiolytic (emotional blunting  no disinhibition), sedative, dissociative feeling (altered state), Reduces pain sensitivity, neuroprotective, distorts visual acuity

antidepressant

GluN2A

increase long term depression

short-term memory

GluN2B (glutamate)

long-term memories

GluN2C

no info

GluN2D

long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning

NMDA

antidepressant

bladder issues

(MK-801)

AMPA

AMPA

motor coordination disruptions, convulsions, and neurotoxicity, enhance cognition and memory, to produce antidepressant-, antianhedonic-, and anxiolytic-like effects, and to have neurotrophic and neuroplasticity-promoting activities. increase levels of BDNF in the hippocampus and to stimulate hippocampal neurogenesis

high-impact AMPAR PAMs decrease both deactivation and desensitization together to enhance and prolong synaptic currents

rapidly-acting antidepressant effects of the NMDA receptor antagonist ketamine appear to be mediated through indirect/downstream activation of AMPARs

antidepressant-like effects in animals are blocked by the AMPAR antagonist NBQX

anticonvulsant

neuropathic pain

sedation

GluA1

centrally involved in synaptic plasticity. Expression of the GluR1 gene is significantly reduced in the human frontal cortex with increasing age

GluA2

regulation of AMPA receptor properties and synaptic plasticity/regulates metabotropic glutamate receptor-dependent long-term depression

GluA3

RNA editing allow faster recovery from desensitization therefore allows continue response to stimulant

GluA4

Metabotropic glutamate  receptor

mGluR5

nootropic and antipsychotic effects

reduce drug self-administration regardless of dose

learned helplessness

mGluR3

sedative, neuroprotective, anti-addictive and anticonvulsant

anxiolytic effects without producing sedation + slightly reduce cognitive performance + inhibiting the development of tolerance to morphine + relieving the symptoms of withdrawal from chronic use of both nicotine and morphine + reducing the effects of 5HT2A agonist hallucinogens + noticable reduce of yohimbine-induced stress response

antidepressant

antidepressant increase behavioral effects of hallucinogenic drugs increasing analgesic effects of μ-opioid agonists modulating dopamine receptor function

antagonizing give anxiolytic effect too but its deferent then the  anxiolytic effect produced by agonists

antidepressant and anxiolytic + boost release of dopamine and serotonin in specific brain areas

mGluR2

antipsychotic and anxiolytic

auto receptor

decreases cocaine self-administration in rats, with no effect on food self-administration

mGluR1

block adrenergic receptor activation in neurons

neuroprotective agent for the treatment of stroke.

analgesic

Mice lacking mGluR1 had impaired motor functions, characterized by impaired balance. In the Morris watermaze test, an assay for learning abilities, those mice needed significantly more time to successfully complete the task

mGluR1a

significantly inhibited sexual motivation

mGluR4

treatment of Parkinson's disease

mGluR6

response to light

mGluR7

inhibit cocaine and alcohol self-administration

mGluR8

anticonvulsant + treatment for hyperalgesia

Ionotropic glutamate receptor/Kainate

GluR5

protect against seizures

neuroprotective + anticonvulsant + antihyperalgesic + analgesic + anxiolytic

suppresses both the withdrawal symptoms from opioids and the development of tolerance

GluR6

associated with nonsyndromic autosomal recessive mental retardation

GluR6 KO mice exhibited less anxious or more risk-taking type behavior and less despair-type manifestations, and they also had more aggressive displays

GluR7

RNA editing

KA1

regulation of antidepressant treatment-response like citalopram

KA2

no info in the first 100 Google search result just they linked to "Intracellular Trafficking"

GABA

α

sedative + relaxing

antidepressant

stimulant

α1

induce sleep

sedative or amnestic

α2

anxiolytic

α3

α4

amnesia

ataxic, sedative, and analgesic effects

decreases their free consumption of and preference for alcohol

α5

do not have convulsant or anxiogenic effects but instead show cognitive- and memory-enhancing or nootropic-like effects

α6

β

sedative + relaxing

antidepressant

stimulant

β1

β2

anesthetic

β3

sedation

α-ρ1

α-ρ2

SSRIs like effect

increase serotonin

α-ρ3

γ1

γ2

elevated anxiety + altered emotional behavior reminiscent of melancholic depression + depression related anhedonia in the sucrose consumption test

elevated serum corticosterone levels

epilepsy

γ3

Autism and autism spectrum disorders

δ

Knockout females, but not males, show improved fear conditioning

Mice lacking the δ subunit show reduced sensitivity to neuroactive steroids

ε

θ

π

overexpressed in pancreatic adenocarcinomas

opioid

DOR δ1

euphoria

physical dependence

DOR δ2

KOR κ1

analgesic, anxiogenic, and dissociative/hallucinogenic

KOR κ2

KOR κ3

MOR μ1

respiratory depression

physical dependence

Opioids down-regulate the HPA-axis to produce near-castrate testosterone levels, while also suppressing adrenocorticotropic hormone secretion from the anterior pituitary (this lead to decrease libido etc,, effect of low T)

Restless legs syndrome

increased sensitivity to physical touch and pain

MOR μ2

euphoria

MOR μ3

NOR

depression

development of tolerance to μ-opioid agonists

NOR ORL1

ZOR

tissue growth

NOP

treatments for depression and Parkinson's disease

trace  amine receptors

0.71 (dopamine)

TAAR1

decrease Serotonin, Noradrenaline, Dopamine, reuptake inhibition

TAAR2

not about depression

TAAR5

TAAR6

TAAR8

TAAR9

COMT

convert  catecholamine's to rubbish

stop convert  catecholamine's to rubbish

+levodopa

fos

ΔFosB

happiness seeking behaviors (craving)

anti-craving effect

c-Fos

don't increase the chronic induction of ΔFosB

increase the chronic induction of ΔFosB

adenosine

A1

anticonvulsant and analgesic

feel more energized and awake + heart-pounding effects

A2A

wakefulness-promoting effects, Antagonism of A2A receptors in the ventrolateral preoptic area reduces inhibitory GABA neurotransmission to the tuberomammillary nucleus, a histaminergic projection nucleus that activation-dependently promotes arousal

A2B

provide protection from ischemia (lack of oxygen due to blocked blood supply)

promotes progression of human oral cancer

anti-inflammatory

inhibits release of interleukins that is involved in the development of spatial memories

A3

anti-inflammatory

cAMP

stimulant

oxidants

decrease cell death due oxidative stress

smooth skin (anti-aging effect)

PDE

1

increase cAMP used in: Parkinson's disease, Alzheimer's disease, Epilepsy

2

increase cAMP used in: improving memory

3

increase cAMP used in: acute heart failure and cardiogenic shock

4

increase cAMP used in: precognitive (including long-term memory-improving), wakefulness-promoting, neuroprotective, and anti-inflammatory effects

5

increase cAMP used in: erectile dysfunction

7

increase cAMP used in: anti-inflammatory and neuroprotective

induction of dopaminergic neurogenesis

10

motor and cognitive deficits and increased anxiety

increase cAMP used in: erectile dysfunction, treatment for schizophrenia

9

increase cAMP used in: improve learning and memory

11

poorly understood, in part due to the lack of selective inhibitors

Oxytocin

Oxytocin

love (mostly because androgen Neurotransmitter "Oxytocin" have wake biding affinity to Vasopressin 1A)

Vasopressin

1A

social recognition (mostly this is empathy of SSRIs + testosterone directly suppresses oxytocin in mice)

Romantic attachment (physical and physiological)

emotional talk + increase ability to trust others + increase generosity

Oxytocin evokes feelings of contentment, reductions in anxiety, and feelings of calmness and security when you are with your friend

reduced anxiety-like behavior

greatly impaired social recognition abilities

social isolation

deficits in circadian rhythms and olfaction

1B

aggression

ability to recognize recently investigated mice

reduced social motivation or awareness

2

antidiuretic

Orexin

OX1

happiness

happiness seeking behaviors

wakefulness + regulates energy expenditure + increase appetite + body temperature and locomotion

OX2

P-glycoprotein

prevent drugs from across BBB (involved in tolerance)

cause some peripherally acting drugs to have central nervous system action too

estrogen receptor

ERα

induced increase in SHBG which lower free testosterone + upregulation of gonadal testosterone production due to reduced negative feedback by androgens on the hypothalamic–pituitary–gonadal axis

undersized testes, stimulate cell proliferation in breast tissue

maintenance of bone integrity

antidepressant-like effects

Erβ

anti-proliferative in reproductive tissue

anxiolytic

antidepressant, anxiolytic, cognitive-enhancing, and stress-relieving

up-regulates oxytocin receptors

increase sexual motivation

cognitive impairment , and development of AD pathology

Abnormalities in gene expression associated with ER-β have also been linked to autism spectrum disorder

GPER

GPER and ERβ play a modulator role in breast development, ERα is the main receptor responsible for estrogen-mediated breast tissue growth

anxiogenic

Lordosis to front

Estrogen-related receptor

ERRα

ERRalpha KO mice:-reduced body weight, resistant to high-fat diet induced obesity

ERRβ

ERRβ Null Mice: show severely impaired placental formation.

ERRγ

protect pre-menopausal women from age-related hearing loss

Membrane estrogen receptor

Gq-mER

no info

Erx

ER-X

Androgen receptor

AR

have important role in prostate cancer

GPRC6A

mediate rapid, non-genomic prostate cancer cell responses to testosterone

increase skeletal muscle strength, indicating potential anabolic effects, implicated in the antigonadotropic effects of androgens

14nM(Kd)

ZIP9

increase skeletal muscle strength, indicating potential anabolic effects, implicated in the antigonadotropic effects of androgens

progesterone receptor

PR-A

serve to antagonize the effects of PR-B

delayed but otherwise normal mammary ductal development at puberty

impaired lobuloalveolar development of the mammary glands

PR-B

positive regulator of the effects of progesterone

PR-C

mPRγ

no info

mPRδ

mPRα

mPRβ

mPRϵ

AdipoR1

AdipoR2

Glucocorticoid receptor

LINKED TO PTSD

Mineralocorticoid

Cannabinoid

CB1

anxiolytic

increase appetite, novelty, appreciation for food, music, art, analgesic, decrease short-term memory

CB2

anti-inflammation

preventing cognitive impairment and loss of neuronal markers

anti-cancer properties

NAGly (GPR18)

anti-inflammatory

without producing any psychoactive effects

GPR55

altered blood pressure regulation

GPR119

body weight loss by reduction in food intake

Neuropeptide Y receptor

Y1

regulation of appetite, anxiety, BIBP-3226 has anxiogenic and anorectic effects

Y2

reducing alcohol consumption in addicted rats[6][7] and anxiolytic effects

Y4

Y5

anorectic, antidepressant and anxiolytic effects

peroxisome proliferator-activated receptor gamma

PPAR-γ

uprgulate SERT + increase production of serotonin (the result is antidepressant effect)

Melanocortin

MC1R

hyperpigmentation primarily of the hair and skin

decrease sensitivity to pain

MC2R

upregulates levels of cAMP by activating adenylyl cyclase

MC3R

increased fat mass despite decreased food intake

MC4R

powerful  treatments for  female and male sexual dysfunction

via activation of the central oxytocin system, have been found to promote pair bond

produce pronounced antidepressant- and anxiolytic-like effects

Obesity

MC5R

male mice decreases aggressive behavior, promotes defensive behavior and encourages other male mice to attack MC5R-deficient males through pheremonal signals

decreased production of sebum

Thyroid hormones

T3

weight loss, tremor, headache, upset stomach, vomiting, diarrhea, stomach cramps     nervousness, irritability, insomnia, excessive sweating, increased appetite, fever, changes in menstrual cycle, sensitivity to heat

ZINC RECEPTOR

GPR39

SSRIs upregulate this (involved in the antidepressant response)

Histone deacetylase

HDAC2

treatment for Parkinson's Disease

prevented cognitive and behavioral impairments in mice with Alzheimer's Disease

HDAC1

no info in Wikipedia

HDAC3

HDAC4

regulates bone and muscle development

HDAC5

involved in memory consolidation

HDAC6

Mutations in this gene have been associated to Alzheimer's disease

HDAC8

HDAC9

HDAC10

HDAC10 has been shown to interact with Histone deacetylase 2, and Nuclear receptor co-repressor 2

HDAC11

upregulation of HDAC11 expression has also been seen in various cancer cells

Sirtuin

implicated in influencing cellular processes like aging, transcription, apoptosis, inflammation implicated in influencing cellular processes like aging, transcription, apoptosis, inflammation ( nicotinamide inhibit this)

COX

COX-1

COX-2

suppressing inflammatory neurodegenerative pathways in mental illness

Neurotensin

NTS1

blocked the effects of stimulant drugs including MDMA

NTS2

GHB receptor

GPR172A

do not produce a sedative effect, instead causing a stimulant effect followed by convulsions at higher doses, thought to be mediated through increased Na+/K+ current and increased release of dopamine and glutamate

Angiotensin II

AT1

increase vasoconstriction, aldosterone synthesis and secretion, increased vasopressin secretion

reduce fear memory recall

AT2

inhibition of cell growth

Over expression of the AT2 receptor down-regulated the AT1 receptor

Decrease of dopamine synthesis

AT3

no info in the first 100 Google search result

AT4

induce release of oxytocin (anxiolytic effect)

enhances learning and memory and cognition

vitamin D receptor

VDR

increase calcium absorption

loss of bone density

regulates the expression of more than 900 genes  (cell growth and development, immune function, and metabolic control)

Melatonin

MT1

MT1 receptor knockout mice exhibit depression-like behaviour and reduced mobility in the forced swim test compared to wild-type mice.

MT2

MT2 receptor knockout mice do not exhibit luzindole-mediated antidepressant-like actions, as seen in wild-type mice.

GPR50

Physiological function of GPR50 remains unclear, although studies implicate the receptor in energy homeostasis [12].

calcium

α2δ-1

anticonvulsant, analgesic, and anxiolytic effects (opiates and benzo-like effect)

Sodium

Nav1.2

mutations in this gene have been linked to several seizure disorders and autism, infantile spasms bitemporal glucose hypometabolism , and bipolar disorder

Nav1.3

anti-Neuropathic pain

Nav1.4

Mutations in the gene are associated with hypokalemic periodic paralysis, hyperkalemic periodic paralysis, paramyotonia congenita, and potassium-aggravated myotonia

Nav1.5

cardiac diseases is associated with mutations (Long QT syndrome type 3)

Nav1.8

treatment of chronic pain

Nav1.9

pain relief

inti-inflammatory

Potassium channels

K2P2.1

anxiolytic and antidepressive effect

Kv7.1

Mutations in the gene can lead to a defective protein and several forms of inherited arrhythmias as Long QT syndrome, Short QT syndrome, and Familial Atrial Fibrillation

Kv7.2

anticonvulsants

G protein-coupled receptor kinase

GRK6

upregulate D2/D3 receptor

upregulate mu-opiates receptors

GRK2

The agonist-dependent phosphorylation of the rat D1A receptor was substantially increased

upregulate β2 adrenergic receptors

upregulate mu-opiates receptors

GRK3

upregulate mu-opiates receptors

upregulate KOR-opiates receptors

GRK5

Retinoid receptor

RAR-alpha 1

Knock-out mice studies showed that a deletion in one of the copies of the RARA gene did not create any observable defect, while deletion of both copies shoes symptoms similar to that of Vitamin A deficiency. This proved that all 3 subtypes of RARs work redundantly.

Ro41-5253 (1 mg/kg) treatment downregulated RARα protein expression in hypothalamic PVN and hypothalamus, and increased the protein levels of BDNF, PSD95, SYP and MAP2 in the hippocampus. We concluded that Ro41-5253 had antidepressant-like effects on CUMS rats by downregulating HPA axis hyperactivity and improving the hippocampal neuronal deficits

as the absence of retinoid receptors results in a reduced expression of the DA D2 receptor/mutations for the acid retinoic receptors demonstrated in mice could reduce expression of D1 and D2 receptors and do impair dopamine signaling

RAR-alpha 2

RAR-alpha 3

RAR-beta

limits growth of many cell types by regulating gene expression

associated with cancer onset/progression

RAR-gamma

shown to interact with NCOR1

Depression, Mood changes, Suicidal ideation

anti-cancer

RXR

downregulation of thyroid stimulating hormone

significant increase in cholesterol levels and a decrease in total thyroxine levels

RXR-alpha

regulating their transcription (unknown what it is)

RXR heterodimer in the absence of ligand is bound to hormone response elements complexed with corepressor protein. Binding of agonist ligands to RXR results in dissociation of corepressor and recruitment of coactivator protein, which, in turn, promotes transcription of the downstream target gene into mRNA and eventually protein.

RXR-beta

involved in mediating the effects of retinoic acid (RA). This  increasing both DNA binding and transcriptional function on their respective response elements

Induction of apoptosis (associated to RARa activation)

RXR-gamma

the antiproliferative effects of retinoic acid (RA).

Adapalene (CD-271) is a dual RAR and RXR agonist, used in the treatment of acne (which make sure that rxr is upregulate ht1a presynpatic receptors and dopamine 2)

very strong acne treatment

suppression of thyroid function

ablation of Rxrgamma in mice leads to depressive-like behaviors including increased despair and anhedonia, which were accompanied by reduced expression of dopamine D2 receptor in the shell of nucleus accumbens (NAc) and altered serotonin signaling (proberly increase singling of serotonin)

Nuclear receptor

NCOR1

assists nuclear receptors in the down regulation of target gene expression (unknown what it is)

Loss of function of this protein significantly increases the strength and power of mouse muscles

NCOR2

Neurokinin

TACR1

has been associated with the transmission of stress signals and pain

99% human receptor occupancy might be required for consistent psycho-pharmacological or other therapeutic effects

prevent chemotherapy-induced nausea and vomiting

anti-pain

TACR2

antidepressant and anxiolytic

treatment of asthma

TACR3

dose-dependently suppress luteinizing hormone (LH) secretion, though not that of follicle-stimulating hormone (FSH), and consequently to dose-dependently decrease estradiol and progesterone levels in women and testosterone levels in men

how to use:

online:

for android users use google sheets for android
for IOS  users use google sheets for ios
for desktop use this link for google docs (it will open the app in android)
that link will changed when new version made

offline:

download the excel file (2021-8-20)

run it with excel (the best experience)

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