OPIATES:

Azidomorphine - 40x potency of Morphine with high affinity to μ
Myrophine* - Morphine + 3-benzyl & 6-myristyl chain and acts as a prodrug to M. Has a slow onset of effects and longer duration but reduced potency. Does NOT produce addiction or dependance regardless of dose.
6-MDDM - 80x potency of Morphine, faster onset and less body load
Dipropanoylmorphine - Ester of M used to treat severe pain. Rarely used but considered to be safer and less adictive than M. As such carries less side effects, such as euphoria. Slower acting, longer lasting and slightly more potent than M.
Methyldihydromorphine - Related to heterocodeine not dihydrocodeine. Could be 6-9x potency of morphine and a drug of abuse.
Diacetyldihydromorphine - Occasionally used an alternative to diamorphine, of which it is faster acting, longer lasting and has less side effects such as euphoria and addiction. However it is equipotent with morphine.
Heterocodeine - Reverse isomer of codeine. 6x potency of M, while Codeine is a prodrug, HC is a direct agonist.
Methyldesorphin - 15x potency of M. Is found in Krokodil
14-Cinnamoyloxycodeinone - 100x potency of M, interesting.
3-Acetyloxymorphone - Acetylated analogue of OM
Oxymorphazone - half potency as OM but higher doses last up to 48hrs - irreversible full μ agonist
Chloroxymorphamine - Derivative of OM and irreversible full agonist
Nicomorphine - 2-3x the potency of M and commonly prescribed in German speaking countries
Apomorphine -
Metamizol -
Metopon - Methylated Hydromorphone, less potent. Interesting though, could have more euphoria
14-Phenylpropoxymetopon - 2000+x potency of M, when injected into spine up to 1,000,000x. 14-MOP has ceiling effect on respiratory depression (!!) but 14-PPOP untested
MT-45 - 80% of M. mixed ant.-ag. and mild NMDA antagonist
Tapentadol - μ & σ agonist & SNRI. Potency in between M & Tram.
Ciramadol - Opioid related to PCP, Tramadol & Tapentadol. mixed ant.-ag. for μ, low abuse potential and ceiling on respiratory depression.
7-Spiroindanyloxymorphone - odd OM analogue, selective d agonist
Oxymorphol - 6-hydrogenated OM, coming soon...
Pentamorphone - few x stronger than fent. short duration but low respiratory depression.
Morphinan-6-one (MR-2096) - OM analogue at roughly 5-7mg dosage. RC. FULL NAME: (N-tetrahydrofurfuryl)noroxymorphone
Hydromorphinol - Derivative of M but more potent, with a steeper dose-response curve and a longer half life. Script in Sweden.
RAM-378* - N-Phenethyl analogue of Hydromorphinol. It is probably more potent as a result.
Ro4-1539 (Furethylnorlevorphanol) - 30-60x the potency of M. One of the more potent u agonists from the Morphans.
Carfentanil - 100x potency of fent., 10000x the potency of M. Used in spetznaz hostage crisis. 10,000x potency of M. Activity in humans starts at 1μg.
Lofentanil - more potent and with a longer duration than carfentanil.
Remifentanil - Potent ultra short acting fent. analogue. Potency from between 20 and 100ug. Used in medicine as an anaesthetic under Ultiva.
3-Methylfentanyl - 400-6000x potency of M depending on isomer (cis-iso more potent)
Ohmefentanyl - 6300x morphine at it's most active isomer. Analogues of this are even stronger with one possessing 30,000x the potency of M.
Alfentanil - 1/4 the potency and 1/3 the duration of fent but 4x quicker onset. The businessman's lunch of opiates.
Betahydroxythiofentanyl - one of the more favoured fent. analogues by addicts, implying euphoria.
Sufentanil - 5-10x potency of fent.
R-30490 - analogue of carfentanil. Most selective μ agonist of all fentanyl analogues
Mirfentanil - fent. analogue with strong selevtivity over μ. Lower doses it antagonises effects caused by lesser opioids but at higher doses is resistant to antagonists, suggesting it has non-opioid mechanisms.
7-PET - 300x potency of M, 3-OH derivative is 2200x potency of M. Unscheduled.
Etorphine - 1000-3000x potency of M. μ, κ & δ opioid agonist. weak affinity for ORL1 nociceptin/orphanin FQ receptor.
Dihydroetorphine -1000-12000x potency of M depending on RoA. Less addictive than other opiates and is used in a similar fashion to Subutex in China.
Acetorphine - 8700x potency of M
BU-48 - Etorphine derivative. Selective δ agonist and produces only convulsions with slight antidepression.
Etonitazene - 1000-1500x potency of M.
AD-1211 - mixed ant.-ag. similar to Pentazocine. Little development of tolerance or dependance.
AH-7921 - Selective μ agonist, with 80% potency of M. distributed as an RC, TRs show that it has very little euphoria, indicating euphoria comes from somewhere else. Perhaps sigma? Other opioids are heavily potentiated by it. Perhaps μ agonism is purely analgesic and high comes from a combination of μ & δ with each multiplying the affect of the other. This indicates ultimate opiate high would be moderately selective δ agonist
Bromadol (BDPC) - 500-10,000x potency of M. Similar to PCP analogues & -HO bonds within them.
3-HO-TCP - PCP analogue. More glutamergic than the PCP analogue.
3-HO-BCP - substitutes for both cocaine and morphine at ~5mg (made-up)
Ketobemidone - μ opioid antagonist & NMDA antagonist. More addictive than M
Acetoxyketobemidone - Unschedualed analogue of ketobemidone
Bemidone - Analogue of Pethidine but significantly less potent, however it has NMDA antagonism like KetoB.
Dipipadone - Lost Ark of the Covenant.
Phenadoxone - methadone analogue, similar dose to M, lasts 1-4 hours
Levacetylmethadol - Methadone analogue with u agonism and noncompetitive a3b4 NACh antagonism. Brand name Orlaam, prescribed to those unresponsive to methadone or subutex. Long half life (3 days) and heavier affect.
Dimenoxadol - Benzillic Acid derivative related to methadone. Banned due to high abuse potential it seems.
Dimepheptadol - related to methadone, has two isomers which also have two isomers so 6 possible isomers including racemic
Dioxaphetyl butyrate - Banned opioid similar to methadone. Possibly in use or previously in use as a med under the names Amidalgon & Spasmoxal.
IC-26 - Methadone analogue with similar potency but Unscheduled.
Lefetamine - Weak opiate on the same scale as codeine but has DRI properties.
Norpipanone - Was not under international control until case reports of addiction arose.
R-4066 - methadone analogue with 212x the potency but a much shorter duration at 3 hours.
Piminodine - similar dose to M, used in 60's and 70's but was banned. It was probably abused widely.
Anileridine - Another banned pethidine analogue, probably abused. Higher analgesia than Meperidine due to n-aminophenyl group and acts withing 15 mins orally, lasting 2-3 hours.
Benzethidine - 4-phenylpiperidine analogue of pethidine. Probably somewhat more potent and euphoric. Never scripted.
4-Fluoropethidine - In comparison to pethidine, it is 50% less potent as an analgesic but 50% more potent as a DRI. (4-iodo & 3, 4-dichloro only increase these differences)
Furethidine - 4-Phenylpiperidine analogue of pethidine. Probably a lot more potent and abuse prone. Never prescribed.
Carperidine - fairly normal opiate but unused in medicine and currently LEGAL (08/06/2013)
Morpheridine - related to meperidine but 4x the potency and does not cause convulsions
Phenoperidine - 20-200x the potency of Pethidine. Less hypnotic and than morphine but more emetic (nausea). This can be cured by Haloperidol.
Picenadol - Mixed antagonist-agonist, low affinity. Potential for expansion
Allylprodine - Prodine analogue 23x potency of M
Prosidol - Russian Prodine analogue
Picenadol - R isomer (or Levopicenadol) is pure μ agonist while S is antagonist. Racemic is mixed that casues low abuse potential but has low κ activity
Palfium (Dextomoramide) - 3x potency of M but shorter acting. High BA & fast acting, oral feels like shooting. Low LD50 & inconsistent potency (one day you may need 5mg, next day 3mg)
Propiram - Slightly more potent than codeine, 3-6hr duration. mixed μ ant.-ag. favouring agonism. affinity for κ & δ, sigma and nmda. 97% oral BA!
Diampromide - Banned Analgesic related to Propiram. Similar potency to M.
BRL-52537 - Highly potent and selective κ agonist. Neuroprotective.
C-8813 (Thiobromadol) - 591x potency of M. μ agonist & δ antagonist to reduce repiratory depression. Making the drug safer.
Herkinorin - Analogue of Salvinorin A but the complete opposite. 100x higher μ affinity and 50x lower κ affinity. Also; "does not promote the recruitment of β-arrestin-2 to the intracellular domain of the μ-opioid receptor, or induce receptor internalization". This means Herkinorin may not produce tolerance or dependance.
Methopholine - Isoquinilone derivative with same efficacy as codeine. Could produces corneal opacity. Analogues are more potent with 4'-nitromethopholine at 20x codeine.
Nortilidine - Equipotency of M. Opioid activity is in (1S,2R) iso, NMDA antagonism is in (1R,2S) iso. Also acts as a DRI.
O-Desmethyltramadol - metabolite of Tramadol. Considerably more potent than Tramadol. Both (+) & (-) isomers lose SRI function but (-) retains NRI functionality. RC.
SC-17599 - selective μ agonist with little or no affinity for δ & κ. Potency in between pethidine & morphine.
RWJ-394674 - potent and selective δ agonist, however once inside body it is dealkylated to its monodesethyl metabolite RWJ-413216 which is a potent μ agonist with less affinity for δ. δ activity counteracts the respiratory depression the μ causes. Only prominent side effect is sedation (and euphoria!)
TAN-67 - potent and selective δ1 agonist. Has analgesic properties & releases dopamine in the brain. Neuro & cardiac protective properties.
W-15 - 5.4x Morphine. RC.
W-18 - 10,000x potency of M, structure abstract from any other drug. These super potent opioids are used in vetenarian practice for tranquilising elephants.
SoRI-9409 - mixed μ agonist & δ antagonist. moderate analgesia without development of tolerance. Anti-addictive effects for all dopaminergic drugs.
'Synthetic Conotoxin' - Snail toxin derived painkiller 1000x potency of morphine. Non-addictive
Loperamide - Peripheral opioid so it cannot cross BBB. useful anti-Diarrhoea med. When used in conjuction with Quinine or Omerprazole can cross BBB and opioid effects are seen.
BW373U86 - Selective δ agonist at 15x stronger affinity. Analgesic and anti-depressant properties along with BDNF release. Produces convulsions at high doses and reverses respiratory depression produced by μ agonism. Also protects heart muscle cells from death during oxygen deprivation, a result of heart attacks.
DPI-227 - highly selective δ agonist with antidepressant effects but produces fewer convulsions than most other dugs in it's family.
DPI-3290 - Potent δ & μ agonist but produces little respiratory depression.
Bezitramide - (Burgodin?)
Piritramide - 0.65-0.75x M but still effect is strong and long lasting. Has a small but dedicated fanclub on the 'street'
IBNtxA -
Matrine -
Thiambutenes - Dimethyl-TAB, Diethyl-TAB, Ethylmethyl-TAB. Used in vetinary medicine in Japan. Banned in virtually all countried due to high abuse potential. Anticholinergic and antihistamine properties!
Dextropropoxyphene - Low potency opiate not absorbed by CYP2D6. Also is a potent, noncompetitive α3β4 NACh antagonist and a weak SRI.
Deltorphin - High affinity and selectivity, naturally occuring δ opioid agonist.
HZ-2 - κ-opioid agonist, same potency as morphine, long duration, high oral BA
Dermorphin - South American Tree frog skin. Natural opioid peptide. High potency (30-40x M) and selectivity to μ but may be less likely to cause tolerance and addiction.
Thebaine - 6, 14 dimethoxy version of OM. Stimulant rather than analgesic, high dose causes OD
Thebacon - Thebaine analogue and fairly uninteresting
Drotebanol - Morphinan derivative synthesised from Thebaine with analgesic effects several times more potent than codeine but weaker than morphine. Moderately addictive but limited physical dependance. Under Metabanyl when available as a script.
Biphalin - endogenous eptide with high affinity for δ & μ receptors. Potency almost 7x greater than Etorphine and 7000x M. Low side effects; no dependancy caused.
Opiorphin - Endogenous opioid isolated from human saliva.
Met-enkephalin - Opioid Growth Factor (OGF), Endogenous opioid peptide. Primary ligand of the δ receptor along with Leu-enkephalin (high potency and selectivity at δ). Low BA & is metabolised rapidly.
Leu-enkephalin - Endogeneous opioid petide that acts as a δ & μ agonist with strong selectivity for δ.
Casomorphins - opiates found in Cow's milk.
DAMGO - synthetic opiate peptide with high μ selectivity. When administered alongside M for 7 days, M had the same effect at the same dose as the first day. I.e. removes tolerance.
Eseroline - Metabolite of the ACh inhibitor physostigmine but potent μ agonist
Hodgkinsine - alkaloid found in Psychotria colorata plants. Has antiviral, antibacterial and antifungal properties. Also μ opioid agonist & NMDA antagonist.
Mitragynine - Alkaloid in Kratom. Fairly selective μ agonist but little affinity for δ & κ.
7-Hydroxymitragynine - Alkaloid in Kratom. Some 17x potency of M. 30x potency of Mitragynine.

Butinazocine - benzomorphan opioid that was never marketed-----------------\    The Benzomorphans have
Carbazocine - benzomorphan opioid that was never marketed 		    \   to be my favourite structures.
Etazocine - partial opioid agonist with mixed ant.-ag. effects. low potency  \_ The Cubist narcotics.
Ethylketocyclozocine - partial opioid agonist with mixed ant.-ag. effects	The Picassopiates.
Ibazocine - benzomorphan opioid that was never marketed			        They serve no real function
Moxazocine - 10x potency of M, partial/mixed ant.-ag.			      _ except to look pretty to
Tonazocine - partial agonist at μ & δ, no adverse effects on breathing       /  afficionados such as I.
Volazocine - benzomorphan opioid that was never marketed		    /   As do I to afficionados such
Fluorophen - radioligand, full μ agonist (6x M) & lower affinity for δ     /    as they, and they to afficonados
Zenazocine - partial agonist at μ & δ-------------------------------------/     such as we, and we are such afficionados.

Phenomorphan - 10x potency of Levorphanol.
	└--> N-(2-(2-furyl)ethyl) analogue - 60x Levorphanol
	└--> N-(2-(2-thienyl)ethyl) analogue - 45x Levorphanol
Proxorphan - partial κ agonist, lesser partial μ agonist
Levophenacylmorphan - 10x potency of M
Levofurethylnormorphanol (Ro4-1539) - potent μ opioid agonist 30-60x potency of Levorphanol.
Levomethorphan (+) - NDMA antagonist, σ1 & σ2 sigma agonist, μ, δ & κ opioid agonist.
Levorphanol (+) - μ, κ & δ agonist, 4-8x potency of M, long duration, no cross tolerance with morphine
Norlevorphanol - Opioid analgesic, uninteresting.

IDEA: For potent opioid analogues (C-8813, Bromadol, Etorphine etc.) buy 1-10mg amounts from legitimate research labs for ~$150. BE CAREFUL!!


ANTI-OPIOID - (selective δ antagonists may reduce physical addiction without causing w/d if attatched to an opioid)

Chlornaltrexamine - Irreversible mixed ant.-ag. at μ opioid. 22x more potent than M
Naloxazone - Irreversible μ opioid receptor antagonist
Naloxonazine - Very Potent Irreversible μ opioid antagonist. dimerizes from Naloxazone under acidic conditions
Buprenorphin - Subutex
Levallorphan - μ opioid antagonist, when used with opiate, it potentiates it and removes addiction potential or induces withdrawal in addicts.
Diprenorphine - Strongest opiate antagonist available. 100x potency of Nalorphine. Used to reverse effects of super-potent opioids.
Cyprodime - Selective μ opioid antagonist with no affinity for κ or δ receptors
Xorphanol - mixed ant.-ag. produces convulsions at highest dose tested.
Samidorphan - selective μ antagonist. potential for addiction treatment.
Butorphanol - partial ant.-ag. at μ opioid and competitive antagonist/partial agonist at κ opioid. dysphoria is common at normal dose.
Eptazocine - Japanese κ agonist & μ antagonist
Amiphenazole - treatment for OD. counteracts respiratory depression. If Morphine-N-oxide is taken on this, M's potency will increase.
κ AGONIST OPIATES SUCH AS IBOGAINE ARE OPIATE CURES.
DYNORPHINS - endogenous opioid peptides, primarily k agonists. Useful in the analysis of addiction.
Naltrexone -  Competitive antagonist at μ & κ receptors, and to a lesser extent, δ. Modulation of the dopaminergic mesolimbic pathway makes it good for countering alcohol dependance as well as Opiate addiction. Blocks the euphoric effects of opioids and is used in rapid detoxification and attenuation of withdrawal. If opiates are used simultaneously, oD may occur.
Nalbuphine - μ antagonist, κ agonist. Used as a non-addictive, non-euphoric analgesic.

HALLUCINOGENIC OPIATES - Most opiates are hallucinogenic but this concerns significant affect. Usually this will be due to κ agonism so the 'trip' will be dysphoric. High potential for addiction treatment.

Cyclorphan - mixed antagonist-agonist with affinity for κ
Pentazocine - mixed ant.-ag. (-) is the κ agonist side, the (+) displays 10x the affinity for sigma receptors. NO μ agonism
Phenazocine - related to ^ but stronger analgesic, 4x potency of M
Cyclazocine - mixed ant.-ag.
Dextromethorphan (-) - NMDA antagonist / σ1 & σ2 sigma agonist / a3b4, a4b2, a7 nACH antagonist, (very weak) μ, δ & κ opioid agonist, SERT & NET inhibitor, NADPH Oxidase inhibitor. (Race)Methorphan = racemic
Dextrorphan (-) - NMDA antagonist / σ1 & σ2 sigma agonist / a3b4, a4b2, a7 nACH antagonist, L-Type voltage-gated calcium channel (LVGCC) blocker, SRI.
Nalbuphine - mixed ant.-ag. as is common with this class, there occurs analgesia with no addictive properties.
Dezocine - Mixed ant.-ag. with high κ antagonism. Low dose=euphoria (μ)   High dose=dysphoria (κ). Wierd structure
Oxilorphan: μ antagonist & weak partial κ agonist
8-Carboxamidocyclazocine (8-CAC) - κ & μ agonist, long duration.
Bremazocine - κ agonist related to Pentazocine
U-50488 - highly selective κ agonist with analgesic effects
ICI-199,441 - high potency, highly selective κ agonist with analgesic effects
Metazocine - analgesic; mixed ant.-ag. at μ, activity also at κ and sigma
Cyprenorphine - Buprenorphine analogue, ant.-ag. effects but with higher affinity towards κ.
18-Methoxycoronaridine - Ibogaine derivative, selective α3β4 nicotinic antagonist, however no affinity for α4β2, NMDA or seretonin. Retains modest affinity at μ & κ opioid.
Ibogaine - Addiction CURE. HT2a agonist, κ opioid agonist, NMDA antagonist
Noribogaine - Metabolite of Ibogaine. Potent SRI, κ antagonist, weak μ full agonist
Voacangine - precursor to Ibogine used by iboga plant. Displays similar effects towards addiction as Ibogaine.
Salvinorin A - Highly potent κ agonist and even more potent D2 partial agonist. Use in therapy for addiction.
Salvinorin B ethoxymethyl ether - semi-synthetic analogue of Salv. A. Longer duration @ ~3hrs, active at 50ug & 3000x (!) selectivity over μ & δ
Salvinorin B methoxymethyl ether - Similar to ^^ but less selective. 5x potency as Salvinorin A. Deacetylised from Salvinorin A.
Enadoline - Highly selective κ agonist. Produces visual distortions, dissociation and of course dysphoria similar to Salvia.
U-69,593 - Potent and selective κ1 agonist. Produces; antinociception, anti-inflammation, anxiolysis (low doses), respiratory depression & diuresis. Also inhibits periphery oxytocin secretion. Not sure if hallucinogenic.
Tifluradom - Benzo derivative but without GABAa agonism. Instead selective κ agonism.
Alazocine - σ1 agonist, κ opioid agonist & slight NMDA antagonist


MORPHINANS

(Race)Methorphan: L(eft) (+) Levomethorphan >< Dextromethorphan (-) D(exter) --> l=OPIATE >< d=HALLUCINOGENIC OPIATE
	   └--> Racemic mix of both isomers, embodying their properties.
Morphinan (Racemorphan):    l (+) Levorphanol >< Dextrorphan (-) d --> l=OPIATE >< d=HALLUCINOGENIC OPIATE
		 └--> Racemic mix of both isomers, embodying their properties.
(Race)Allorphan:  l (+) Levallorphan >< Dextrallorphan (-) d --> l= ANTI-OPIOID >< d=NMDA ANTAGONISTS
	  └--> Racemic mix of both isomers, embodying their properties.
3-Hydroxymorphinan: l (+) Norlevorphanol >< Nordextrorphan (-) d --> l=OPIATE >< d=NOOTROPIC
	   └--> Racemic mix of both isomers, embodying their properties.
Oxilorphan - HALLUCINOGENIC OPIATE
Phenomorphan - OPIATE
	└--> N-(2-(2-furyl)ethyl) analogue - OPIATE
	└--> N-(2-(2-thienyl)ethyl) analogue - OPIATE
Dimemorfan - SIGMAERGIC DRUG
Levophenacylmorphan - OPIATE
Levofurethylnormorphanol (Ro4-1539) - OPIATE
Xorphanol - ANTI-OPIOID
Proxorphan - OPIATE
Cyclorphan - HALLUCINOGENIC OPIATE
Cyprodime - ANTI-OPIOID
Butorphanol - HALLUCINOGENIC OPIATE
Samidorphan - ANTI-OPIOID


Chitosan - linear polysaccharide that can give Morphine up to 60% BA intranasally. Powdered & the ratio is 1.3g : 6.7g (morpine : chitosan)
BIMU-8 - NOOTROPIC
NMDA antagonists - Inhibit development of tolerance to morphine
Tezampanel - ANXIOLYTIC
Ibudilast - NOOTROPIC
Nuciferine
Tetrahydropalmatine - ANXIOLYTIC
Lofexidine - ANXIOLYTIC
d & l Phenylalanine (DLPA) - Increases dopamine and endorphin levels, reducing opiate tolerance and even providing an analgesic effect of it's own.
CCK ANTAGONISTS
Proglumide - Acts as a d opioid agonist and non selective CCK antagonist. Enhances analgesia produced by opioids and can prevent or even reverse the development of tolerance
Devazepide - No affinity for GABAa, selective CCKa antagonist.
Lorglumide - Selective CCKa antagonist for treatment of gastrointestinal problems and some forms of cancer as well as Opioid interacting properties.



CYTOCHROME P450 INHIBITORS -> In separate file: "enzymes"

NOCICEPTINERGIC DRUGS (ORL-1 ant. & ag.'s)

J-113,397 - Highly selective ORL-1 antagonist. Prevents development of opiate tolerance, stimulates dopamine release, cognitive enhancer
SB-612,111 - Selective ORL-1 antagonist but several times the potency of ^^
MCOPPB - Potent, selective ORL-1 agonist with only moderate affinity for μ, even less for δ & κ. Anxiolytic with no inhibition of memory, motor function or sedation
NNC 63-0532 - Potent, selective ORL-1 agonist.
Ro64-6198 - Potent, selective ORL-1 agonist with 100x selectivity over others. In rats produced anxiolytic but no anticonvulsant effects. Impairs Short term memory & increases appetite. Reduces analgesic effects of M but no preventing tolerance. In primates it showed analgesic behaviour without respiratory depression.
Menabitan - potent cannabinoid receptor agonist with anti-nociceptive effects

ENKEPHALIN PROTEASE INHIBITORS
RB-101*** - Inhibits enzymes responsible for breaking down enkephalin (regulates nociceptin). Weak μ & δ affinity and slight σ1. Potentiates opiates, stops withdrawal symptoms, no addiction potential, produces no respiratory depression. Also exerts very potent antidepressant and anxiolytic effects. Not orally active so analogues vv were developed.
RB-120 - Orally active version of ^^. This is best atm.
RB-3007 - Another Enkeph. PI & Nociceptin antagonist




ANTIHISTAMINES - All First Generation Antihistamines will potentiate opioids.

Diphenhydramine - Removes Nausea effectively, slight potentiation at higher doses
Dimenhydrinate - Similar to DPH, more effective against nausea
Promethazine - 1st Gen. Antihistamine with low hall. dose : effecive therapeutic dose
Hydroxyzine - Also HT2a and D2 antagonist.
Cyclizine - Strong potentiation
Chlorphenamine - SNRI, potentiation present but minimal.
Tripelennamine - weak SDRI with minimal anti-cholinergic effects.
Orphenadrine - NMDA antagonist
Doxylamine
Imipramine - Triple RI, D releaser, ACh M2 antagonist, adrenergic antagonist, low sigma affinity, histamine antagonist, BDNF enhancer (neurogenesis) & μ opioid agonism
Ciproxifan - potent H3 inverse agonist/antagonist, wakefulness and cognitive enhancing effects
A-349,821 - potent H3 antagonist(possible inverse agonist)
Cyproheptadine - Very non-selective antihistamine. Antag. at H1(.06), 5-HT2A(1.7), 5-HT2C(2), 5-HT2B(1.5), mACh (M1-M5 ~7-12), D3(8). Also weak affinity at 5-HT1A, α1, α2, 5-HT6, 5-HT7, D1, D2, 5-HT3, NET.
Dimetotiazine - Japanese Antihistamine and ?serotonin? antagonist.



HISTAMINE AGONISTS (H3 receptor responsible for decreased serotonin/acetylcholine release hence why deleriants (antihistamines) cause hallucinations (similar to schizophrenia))

a-Methylhistamine - selective h3 agonist. lowers blood pressure and heart rate.
Cipralisant - extremely potent H3 agonist, S-isomer is active one. Research has been suspended.
Imetit - h3 agonist
Immethridine - H3 agonist
Methimepip - H3 agonist
Proxyfan - h3 agonist but is "protean agonist". It gives different effects depending on level of activity of H3 receptor in different tissues. From full agonist, to antagonist, to inverse agonist.



CHOLINERGICS

Huperzine A - acetylcholinesterase inhibitor, NMDA antagonist
Tacrine - anticholinesterase & cholinergic agonist. also a histamine N-methyltransferase inhibitor and carries same properties with M as Amiphenazole (ANTI-OPIOID)
Bifemelane - Cholinergic nootropic
AR-R17779 - potent selective full NACha7 agonist
PNU-282,987 - potent selective full NACha7 agonist
Galantamine - reversable cholinesterase inhibitor, Nico. cholinergic receptor modulater
Arecoline - Areca nut alkaloid. Muscarinic ACh partial agonist, M1, 2, 3, 4
Diphenylpyraline - anti-cholinergic, anti-histamine DRI
Donepezil - reversble acetylcholinesterase inhibitor, 100% BA
Physostigmine - reversible cholinesterase inhibitor. Indirectly stimulates nicotinic and muscarinic receptors, also used to cure atropine, scopolamine and other anticholinergic poisoning.
Indeloxazine - S releaser, DRI, NMDA antag., acetylcholine releaser
S-18906 - Ampakine which induces production of BDNF and AMPA-mediated release of noradrenaline and acetylcholine
Alpha-GPC - Potent source of Choline
Ispronicline - Nico. ACh partial agonist, α4β2 subtype selective
WAY-317,538 - potent selective NACh a7 full agonist with nootropic and neuroprotective properties


Muscarine - Along with Muscarinic Acid, active alkaloids found in Amanita Musaria mushrooms. MACh agonist (possibly ant.)