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Opioid Receptor Inhibitors (inhibitors, and modulators)

Opioid receptors have been targeted for the treatment of and related disorders for thousands of years, and remain the most widely used in the clinic. Mu (μ), kappa (κ), and delta (δ) opioid receptors represent the originally classified receptor subtypes, with like-1 (ORL1) being the least characterized. All four receptors are G- protein coupled, and activate inhibitory G-proteins. These receptors form homo- and hetereodimeric complexes, signal to kinase cascades, and scaffold a variety of proteins. www.bocsci.com

PZM21 - CAS 1997387-43-5

Catalog Number: B0084-007152 Price: $149/10 mg; $298/25 mg Molecular Weight: 361.5 Molecular Formula: C19H27N3O2S

Description: PZM21 is a potent Gi activator with exceptional selectivity for μOR (EC50= 1.8 nM) and minimal β-arrestin-2 recruitment.

[D-Ala2]-Leucine - CAS 64963-01-5

Catalog Number: B0084-040423 Price: $388/1 g Molecular Weight: 569.659 Molecular Formula: C29H39N5O7 Description: [D-Ala2]-Leucine enkephalin is a delta opioid used to study the signaling pathway of delta opioid receptors.

(+)- - CAS 519-02-8

Catalog Number: B0084-070319 Price: $299/2 g Molecular Weight: 248.36 Molecular Formula: C15H24N2O Description: Matrine((+)-Matrine) is an found in plants from the Sophora family, which has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor agonist.

Asimadoline - CAS 153205-46-0

Catalog Number: B0084-071264 Price: $399/50 mg Molecular Weight: 414.549 Molecular Formula: C27H30N2O2 Description: is a κ opioid receptor agonist with less brain-penetrant ability. Asimadoline is the potential treatment of irritable bowel syndrome.

Mitragynine - CAS 4098-40-2

Catalog Number: B0084-071458 Price: $395/250 mg Molecular Weight: 398.503 Molecular Formula: C23H30N2O4 Description: is an indole alkaloid isolated from the plant , and acts as an opioid receptor agonist with preference for μ-opioid receptor. It is a neurochemical that exhibits stimulatory, antinociceptive, and -like effects.

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Naloxegol oxalate - CAS 1354744-91-4

Catalog Number: B0084-465947 Price: $229/100 mg Molecular Weight: 741.82 Molecular Formula: C36H55NO15

Description: oxalate is a CYP3A4 enzyme inhibitor, is a peripherally-selective , for the treatment of opioid-induced constipation.

LY2795050 - CAS 1346133-08-1

Catalog Number: B0084-474497 Price: $199/5 mg Molecular Weight: 407.89 Molecular Formula: C23H22ClN3O2

Description: LY2795050, a κ-opioid Receptor antagonist, has been found to be effective in imaging KOR behaving as a PET tracer. IC50: 0.72 nM and 25.8 nM for κ-opioid Receptor and κ-opioid.

LY-2456302 - CAS 1174130-61-0

Catalog Number: Molecular Weight: 418.5 Molecular Formula: C26H27FN2O2 Description: LY-2456302, also called as CERC-501, is a potent, highly selective and centrally- penetrant kappa opioid receptor antagonist(Ki= 0.807 nM)with favorable pharmacokinetic and pharmacodynamic properties to evaluate the role of KOR in preclinical models of alcoholism.

Hemorphin-7 - CAS 152685-85-3

Catalog Number: Molecular Weight: 997.11 Molecular Formula: C49H64N12O11 Description: -7, a hemorphin peptide with antinociceptive and antihypertensive effects, is an endogenous derived from the β-chain of hemoglobin. Hemorphin peptides activates opioid receptors and inhibiting angiotensin-converting enzyme (ACE). The much lower affinity of hemorphin- 7 for μ-receptors as compared to other opioid peptides may be

compensated by its much higher plasma concentration, resulting in biological effects of comparable magnitude.

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[(pF)Phe4]Nociceptin(1-13)NH2 - CAS 380620-88-2

Catalog Number: Molecular Weight: 1399.6 Molecular Formula: C61H99FN22O15

Description: [(pF)Phe4](1-13)NH2 is a highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80), with 8000-fold selectivity over δ, κ, and μ opioid receptors.

BAM 22P - CAS 76622-26-9

Catalog Number: Molecular Weight: 2839.24 Molecular Formula: C130H184N38O31S2

Description: BAM 22P is a potent endogenous agonist peptide for sensory neuron specific receptor (SNSR) (EC50 = 13 and 16 nM for human SNSR3 and SNSR4, respectively). BAM 22P is also a potent opioid agonist (IC50 = 1.3 nM in guinea pig ileum preparation) displaying opioid- and non-opioid receptor mediated antinociceptive effects in vivo.

DAMGO - CAS 78123-71-4

Catalog Number:

Molecular Weight: 513.7 Molecular Formula: C26H35N5O6 Description: DAMGO is a highly selective peptide agonist of the μ opioid receptor.

Dynorphin A - CAS 80448-90-4

Catalog Number: Molecular Weight: 2147.51 Molecular Formula: C99H155N31O23 A is a heptadecapeptide which is derived from the cleavage of

Description: and found widely distributed in the central nervous system. It acts as an endogenous kappa receptor agonist with nanomolar binding affinity. It also activates human novel opioid receptor-like receptor of ORL1. It is resistant to enzymatic degradation and may has antinociceptive functions.

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PL 017 - CAS 83397-56-2

Catalog Number: Molecular Weight: 535.64 Molecular Formula: C29H37N5O5

Description: PL 017, a analog, is a selective μ opioid receptor agonist (IC50= 5.5 and > 10000 nM for inhibition of 125I-FK 33,824 and 125I-DADLE binding to μ and δ sites respectively). Although the affinity of PL017 for µ-sites is lower than that of , PL 017 is more potent than morphine in all in vitro studies, suggesting a difference in the way in which peptide and alkaloid activate µ-receptors.

DPDPE - CAS 88373-73-3

Catalog Number: 645.79 C30H39N5O7S2 Molecular Weight: Molecular Formula: Description: DPDPE, a selective δ-opioid receptor agonist peptide, has been found to exhibit antinociceptive actions.

DADLE - CAS 63631-40-3

Catalog Number:

Molecular Weight: 569.66 Molecular Formula: C29H39N5O7 Description: DADLE is a prototypical δ-opioid receptor agonist with antinociceptive activity. It also exhibits activity at the μ-opioid receptor.

ICI 174,864 - CAS 89352-67-0

Catalog Number:

Molecular Weight: 691.87 Molecular Formula: C38H53N5O7 Description: ICI 174,864 is a potent and highly selective δ opioid antagonist. It shows partial agonist in vitro activity at δ receptors at high concentrations.

CTAP - CAS 103429-32-9

Catalog Number:

Molecular Weight: 1104.32 Molecular Formula: C51H69N13O11S2 Description: CTAP has been found to be a selective μ-opioid receptor antagonist.

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Nor-Binaltorphimine dihydrochloride - CAS 113158-35-3

Catalog Number: Molecular Weight: 734.71 Molecular Formula: C40H43N3O6.2HCl Description: Nor- dihydrochloride is a potent and selective kappa opioid receptor antagonist.

Nalbuphine hydrochloride - CAS 23277-43-2

Catalog Number: Molecular Weight: 393.9 Molecular Formula: C21H27NO4.HCl Description: hydrochloride is the hydrochloride salt form of Nalbuphine, an agonist at κ-opioid receptors and an antagonist or partial agonist at μ-opioid receptors. Nalbuphine is used as a .

Ac-RYYRWK-NH - CAS 200959-47-3

Catalog Number: Molecular Weight: 1012.17 Molecular Formula: C49H69N15O9

Description: Ac-RYYRWK-NH, a hexapeptide, is a partial agonist of the nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptorr (Ki = 0.71 nM), which exhibits selectivity over μ, δ and κ opioid receptors (IC50 > 4000 nM).

Ac-RYYRIK-NH - CAS 200959-48-4

Catalog Number: Molecular Weight: 939.12 Molecular Formula: C44H70N14O9

Description: Ac-RYYRIK-NH may provide a promising starting point for in vivo tests for antagonism of the action of noc/OFQ and for the further development of highly active and specific antagonists.

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Naltrexone - CAS 16590-41-3

Catalog Number: 16590-41-3 Molecular Weight: 341.40 Molecular Formula: C20H23NO4 Description: , also called as Celupan, competitively antagonise μ, κ, δ, and σ-opioid receptors with the effect to reduce the occurrence of addictive behaviours .

Naltrexone HCl - CAS 16676-29-2

Catalog Number: 16676-29-2 Molecular Weight: 377.86 Molecular Formula: C20H23NO4.HCl Description: Naltrexone significantly suppresses ethanol self-administration and prevents ethanol-induced increases in dialysate dopamine levels.

Trimebutine Maleate - CAS 34140-59-5

Catalog Number: 34140-59-5 Molecular Weight: 503.54 Molecular Formula: C22H29NO5.C4H4O4 is an opioid receptor agonist used as spasmolytic agent abdominal pain. Description:

Loperamide HCl - CAS 34552-83-5

Catalog Number: 34552-83-5 Molecular Weight: 513.5 Molecular Formula: C29H33ClN2O2.HCl Description: HCl is an opioid-receptor agonist with an ED50 of 0.15 mg/kg.

ICI 199,441 hydrochloride - CAS 115199-84-3

Catalog Number: Molecular Weight: 427.80 Molecular Formula: C21H25Cl3N2O Description: ICI 199,441 hydrochloride is the hydrochloride salt of ICI 199,441, which is a selective and highly potent κ agonist. It is 146-fold more active than U-50488 in vitro. It has a broad range of effects on the immune system ranging from inflammatory response modulation to opioid and chemokine receptor expression. It has properties.

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SNC 162 - CAS 178803-51-5

Catalog Number: Molecular Weight: 419.61 Molecular Formula: C27H37N3O Description: SNC 162 is a potent and selective non-peptide δ-opioid receptor agonist (Ki = 0.63 nM), displaying > 8000-fold selectivity over μ-opioid receptors. SNC 162 is centrally active following systemic administration in vivo.

ICI 154,129 - CAS 83420-94-4

Catalog Number:

Molecular Weight: 638.83 Molecular Formula: C34H46N4O6S Description: ICI 154,129 is a selective δ opioid antagonist. It is a peptide analog that antagonized the effects of Leu-enkephalin.

Alvimopan - CAS 156053-89-3

Catalog Number: 156053-89-3 Molecular Weight: 424.53 Molecular Formula: C25H32N2O4 Description: is a novel, oral, peripherally acting antagonist of the mu opioid receptor, which can help gastrointestinal recovery after surgery. Phase III IC50: Mu-type opioid receptor= 1.7 nM

Alvimopan dihydrate - CAS 170098-38-1

Catalog Number: 170098-38-1 Molecular Weight: 460.57 Molecular Formula: C25H32N2O4.2H2O Description: Alvimopan dihydrate is a novel, orally available peripherally restricted opioid antagonist with low systemic absorption. It accelerates the gastrointestinal recovery period with most common side effects in chronic pain patients with OBD were abdominal pai

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Met-Enkephalin - CAS 58569-55-4

Catalog Number: 58569-55-4 Molecular Weight: 573.66 Molecular Formula: C27H35N5O7S

Description: Met-Enkephalin is synthetic opioid peptides that has opioid effects of a relatively short duration.

[Leu5]-Enkephalin - CAS 58822-25-6

Catalog Number:

Molecular Weight: 555.63 Molecular Formula: C28H37N5O7 Description: [Leu5]-Enkephalin is an endogenous opioid agonist peptide with morphine-like activity. It inhibits electrically stimulated contractions in mouse vas deferens (IC50 = 11.4 nM).

Meptazinol Hydrochloride - CAS 59263-76-2

Catalog Number: 59263-76-2 Molecular Weight: 269.81 Molecular Formula: C15H23NO.HCl Description: is a unique centrally active opioid analgesic, which inhibits [3H]-

binding with IC50 of 58 nM.

[Arg14,Lys15]Nociceptin - CAS 236098-40-1

Catalog Number: Molecular Weight: 1909.18 Molecular Formula: C82H137N31O22

Description: [Arg14,Lys15]Nociceptin behaves as a highly potent agonist of the OP(4) receptor (EC50 = 1 nM) and is able to produce long-lasting effects in vivo, compared with the natural ligand NC. It exhibits > 875-fold selectivity over opioid receptors (IC50 values are 0.32, 280, > 10000 and 1500 for NOP, μ, δ and κ receptors respectively).

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[Nphe1]Nociceptin(1-13)NH2 - CAS 267234-08-2

Catalog Number: Molecular Weight: 1381.6 Molecular Formula: C61H100N22O15

Description: [Nphe1]Nociceptin(1-13)NH2 acts as the first truly selective and competitive antagonist and is devoid of any residual agonist activity. It binds selectively to recombinant nociceptin receptors (pKi = 8.4), and competitively antagonizes the actions of nociceptin in vitro and in vivo.

GR 89696 fumarate - CAS 126766-32-3

Catalog Number: Molecular Weight: 530.4 Molecular Formula: C19H25Cl2N3O3.C4H4O4 Description: GR 89696 fumarate is a potent and selective κ-opioid agonist (IC50 = 0.04 nM)

displaying anti-nociceptive and neuroprotective activity.

DIPPA hydrochloride - CAS 155512-52-0

Catalog Number: Molecular Weight: 484.87 Molecular Formula: C22H23Cl2N3OS.HCl DIPPA hydrochloride is an irreversible and selective antagonist of κ-opioid receptor Description: (KOR).

nor-Binaltorphimine dihydrochloride - CAS 113158-34-2

Catalog Number: Molecular Weight: 734.72 Molecular Formula: C40H43N3O6.2HCl Description: nor-Binaltorphimine dihydrochloride is a selective κ-opioid receptor antagonist.

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BW 373U86 - CAS 155836-50-3

Catalog Number: Molecular Weight: 435.61 Molecular Formula: C27H37N3O2 Description: BW 373U86 is a potent and selective non-peptide δ-opioid receptor agonist (Ki = 1.8, 15 and 34 nM for δ, μ and κ receptors, respectively).

BRL 52537 hydrochloride - CAS 112282-24-3

Catalog Number: Molecular Weight: 391.77 Molecular Formula: C18H24Cl2N2O.HCl

Description: BRL 52537 hydrochloride is the most κ/μ-selective and one of the most potent κ ligands.

BMS 986187 - CAS 684238-37-7

Catalog Number: Molecular Weight: 470.61 Molecular Formula: C31H34O4 Description: BMS 986187 is a potent and selective δ-opioid receptor positive allosteric modulator

(EC50 = 30 nM) exhibiting 100-fold selectivity for δ over μ-opioid receptor.

6'-GNTI dihydrochloride

Catalog Number: Molecular Weight: 544.48 Molecular Formula: C27H29N5O3.2HCl Description: 6'-GNTI dihydrochloride is a potent and selective κ/δ-opioid heterodimer receptor agonist (EC50 = 39.8, 112.5 and > 1000 nM for κ/δ, κ/μ and δ/μ, respectively) without effecting on

opioid receptor homodimers (EC50 > 1000 nM). 6'-GNTI exhibits tissue-specific analgesic effects in vitro.

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SCH 221510 - CAS 322473-89-2

Catalog Number: Molecular Weight: 397.55 Molecular Formula: C28H31NO Description: SCH 221510 is a potent and selective nociceptin opioid receptor (NOP) agonist (EC50 = 12, 693, 683 and 8071 nM, and Ki = 0.3, 65, 131 and 2854 nM at NOP, μ-, κ- and δ-opioid receptors, respectively). SCH 221510 exhibits -like activity at doses that have no effect on overt behaviors such as locomotion in vivo. SCH 221510 is used as the therapy of neuropathic and inflammatory pain.

Dynorphin B - CAS 83335-41-5

Catalog Number: Molecular Weight: 1570.85 Molecular Formula: C74H115N21O17

Description: is a 13-residue opioid peptide, which is derived from the cleavage of prodynorphin and found widely distributed in the central nervous system. It acts as an opioid peptide and a κ-opioid receptor agonists. It has been implicated in antinociceptive functions. It has also been used to prime cardiogenesis in pluripotent embryonic stem cells.

ADL5859 HCl - CAS 850173-95-4

Catalog Number: 850173-95-4 Molecular Weight: 428.95 Molecular Formula: C24H29ClN2O3 Description: ADL5859 HCl is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel.

Naloxonazine dihydrochloride - CAS 880759-65-9

Catalog Number: Molecular Weight: 723.69 Molecular Formula: C38H42N4O6.2HCl Description: dihydrochloride is a potent and selective antagonist for μ1 opioid receptors. Studies show that pretreatment with naloxonazine significantly attenuated the acute METH-induced increase in locomotor activity and phosphor-Thr75 DARPP-32 levels.

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CTOP - CAS 103429-31-8

Catalog Number:

Molecular Weight: 1062.28 Molecular Formula: C50H67N11O11S2 Description: CTOP has been found to be an effective and selective μ opioid receptor antagonist and could be used in the treatment of pain.

Naltrindole hydrochloride - CAS 111469-81-9

Catalog Number: Molecular Weight: 450.96 Molecular Formula: C26H27ClN2O3 Description: hydrochloride is a cell permeable, potent and highly selective non- peptideδ opioid receptor antagonist (Ki= 0.02 nM) with 223- and 346-fold greater activity at δ than at μ and κ opioid receptors..

Endomorphin 2 - CAS 141801-26-5

Catalog Number: Molecular Weight: 571.67 Molecular Formula: C32H37N5O5 Description: 2, an andogenous peptide, has high affinity and specificity for the μ- opioid receptor and displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.

ML 190 - CAS 1355244-02-8

Catalog Number: Molecular Weight: 488.58 Molecular Formula: C27H32N6O3

Description: ML 190 is a κ opioid receptor antagonist with IC50 value of 120 nM.

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Nociceptin - CAS 170713-75-4

Catalog Number: Molecular Weight: 1809.04 Molecular Formula: C79H129N27O22 Description: Nociceptin, a 17 amino acid neuropeptide involved in a variety of biological systems, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.

Nocistatin (human) - CAS 212609-11-5

Catalog Number: Molecular Weight: 3561.93 Molecular Formula: C149H238N42O53S3

Description: Nocistatin (human) is a human putative counterpart of nocistatin (bovine). Nocistatin is widely present in the spinal cord and brain, and is a novel bioactive peptide produced from the same precursor as Noc/OFQ. Nocistatin plays important roles in the regulation of pain transmission and learning and memory processes in the central nervous system.

[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 - CAS 213130-17-7

Catalog Number: Molecular Weight: 1367.6 Molecular Formula: C61H102N22O14 Description: [Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2 is the first selective antagonist to prevent the binding of the endogenous ligand orphanin FQ/Nociceptin (OFQ/N) at the orphan opioid-like receptor, demonstrated both in vitro and in vivo. It is selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively).

NocII - CAS 188119-47-3

Catalog Number:

Molecular Weight: 2081.4 Molecular Formula: C92H141N23O28S2 Description: NocII, a heptadecapeptide whose sequence lies immediately downstream of nociceptin, stimulates locomotion in mice, possibly through a novel specific receptor.

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Nociceptin (1-7) - CAS 178249-42-8

Catalog Number:

Molecular Weight: 655.7 Molecular Formula: C31H41N7O9 Description: Nociceptin (1-7), the N-terminal fragment of Nociceptin, antagonizes nociceptin- induced hyperalgesia, with no effect on nociceptin-induced analgesia.

N-MPPP Hydrochloride - CAS 207452-97-9

Catalog Number: Molecular Weight: 358.91 Molecular Formula: C21H26N2O.HCl

Description: N-MPPP Hydrochloride is a high affinity and selective agonist of the κ opioid receptor (KOR-1) with no measured binding at μ or δ sites.

Naltriben mesylate - CAS 122517-78-6

Catalog Number: Molecular Weight: 511.59 Molecular Formula: C26H25NO4.CH3SO3H mesylate is a selective and potent δ-opioid receptor antagonist (Ki= 0.013, Description: 19 and 152 nM for δ, μ and κ receptors respectively).

UFP-101 - CAS 849024-68-6

Catalog Number: Molecular Weight: 1908.19 Molecular Formula: C82H138N32O21

Description: UFP-101 is a potent, selective and competitive silent antagonist for the NOP opioid receptor, displaying > 3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 exhibits antinociceptive activity by opposing the action of nociceptin in vivo.

U-50488 hydrochloride - CAS 67197-96-0

Catalog Number: Molecular Weight: 405.79 Molecular Formula: C19H26Cl2N2O.HCl Description: (±)-U-50488 hydrochloride is a selective κ-opioid agonist with no μ-opioid antagonist effects. (±)-U-50488 hydrochloride blocks Na+ channels at high concentrations.

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(+)-U-50488 hydrochloride - CAS 114528-81-3

Catalog Number: Molecular Weight: 405.79 Molecular Formula: C19H26Cl2N2O.HCl Description: (+)-U-50488 hydrochloride is the less active enantiomer of (±)-U-50488, which is an

opioid receptor agonist.

SB 612111 hydrochloride - CAS 371980-94-8

Catalog Number: Molecular Weight: 454.86 Molecular Formula: C24H29Cl2NO.HCl Description: SB 612111 hydrochloride is a selective NOP receptor antagonist (Ki = 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors, respectively). SB 612111 exhibits antagonist activity at the pronociceptive action of nociceptin in an acute pain model. SB 612111 potentiates the action of

morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model.

SB 205607 dihydrobromide - CAS 1217628-73-3

Catalog Number: Molecular Weight: 506.28 Molecular Formula: C23H24N2O.2HBr Description: SB 205607 dihydrobromide is the first described non-peptide δ1 opioid receptor agonist with high affinity and selectivity for the δ1 subtype (Ki = 1.12, 2320 and 1790 nM at δ1, μ and

κ receptors, respectively).

Endomorphin 1 - CAS 189388-22-5

Catalog Number: Molecular Weight: 610.7 Molecular Formula: C34H38N6O5 Description: Endomorphin 1 is a high affinity (Ki = 360 pM) and highly selective agonist of theμ- opioid receptor with 4000- and 15000-fold preference over δ and κ respectively and displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.

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SNC 80 - CAS 156727-74-1

Catalog Number: Molecular Weight: 449.64 Molecular Formula: C28H39N3O2 Description: SNC 80 is a potent and non-peptide δ-opioid agonist, displaying 2000-fold selectivity over μ-opioid receptors. SNC 80 exhibits antinociceptive as well as pro-convulsant effects in vivo.

Fedotozine tartrate - CAS 133267-27-3

Catalog Number: Molecular Weight: 523.57 Molecular Formula: C22H31NO4.C4H6O6

Description: tartrate is a kappa(1a) opioid receptor agonist.

6 α- - CAS 20410-95-1

Catalog Number: 20410-95-1 Molecular Weight: 329.394 Molecular Formula: C19H23NO4 Description: 6 α-naloxol, a human metabolite of , is an opioid antagonist.

FIT - CAS 85951-63-9

Catalog Number: Molecular Weight: 393.55 Molecular Formula: C23H27N3OS

Description: FIT is a selective and irreversible δ-opioid (DOR) agonist (EC50 = 8 nM).

JTC-801 - CAS 244218-51-7

Catalog Number: 244218-51-7 Molecular Weight: 447.96 Molecular Formula: C26H25N3O2.HCl Description: JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. It is an opioid analgesic drug used in scientific

research.

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BAN ORL 24 - CAS 475150-69-7

Catalog Number: Molecular Weight: 433.594 Molecular Formula: C27H35N3O2 Description: BAN ORL 24, a spiro-isobenzofuran compound, has been found to be a NOP receptor antagonist and could be used to restrain the reduction of locomotor motions with brain permeability. IC50: 0.27 nM.

Cyprodime hydrochloride - CAS 118111-54-9

Catalog Number: Molecular Weight: 391.93 Molecular Formula: C22H30NO3Cl Description: hydrochloride is a selective μ-opioid receptor antagonist from the morphinan family of drugs. Its Ki values are 5.4, 244.6 and 2187 nM for μ-, δ- and κ-opioid receptors respectively. It blocks the μ-opioid receptor without affecting the δ-opioid or κ-opioid receptors. It is useful for scientific research as it allows the μ-opioid receptor to be selectively deactivated so that the actions of the δ and κ receptors can be studied separately. It reduces levodopa-induced dyskinesia in the MPTP-lesioned primate model of Parkinson's disease.

(-)-U-50488 hydrochloride - CAS 114528-79-9

Catalog Number: Molecular Weight: 405.79 Molecular Formula: C19H26Cl2N2O.HCl Description: (-)-U-50488 hydrochloride is the more active enantiomer of (±)-U-50488, which is an

opioid receptor agonist.

Trimebutine - CAS 39133-31-8

Catalog Number: 39133-31-8 Molecular Weight: 387.47 Molecular Formula: C22H29NO5 Description: Trimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.

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Deltorphin I - CAS 122752-15-2

Catalog Number:

Molecular Weight: 768.87 Molecular Formula: C37H52N8O10 Description: I has been found to be an effective δ opioid agonist.

Dermorphin - CAS 77614-16-5

Catalog Number: Molecular Weight: 802.87 Molecular Formula: C40H50N8O10 Description: , a naturally occurring heptapeptide originally found in the skin of amphibians, is a μ-opioid receptor(MOR) agonist with analgesic and antinociceptive effects.

ICI 204,448 hydrochloride - CAS 121264-04-8

Catalog Number: Molecular Weight: 501.84 Molecular Formula: C23H27Cl3N2O4

Description: ICI 204,448 hydrochloride is the hydrochloride salt of ICI 204,448, which is a peripherally acting κ opioid receptor agonist. It does not cross the blood-brain barrier.

Trap 101 - CAS 1216621-00-9

Catalog Number: Molecular Weight: 434.02 Molecular Formula: C24H35N3O2.HCl Description: Trap 101 is a potent and selective nociceptin/orphanin FQ (NOP) receptor antagonist (pA2 = 7.75) with selectivity for NOP receptors over classical opioid receptors (pKi = 8.65, 6.60, 6.14 and < 5 for NOP, μ-, κ-, and δ-opioid receptors, respectively). Trap 101 attenuates motor deficits in a rat model of Parkinson's Disease.

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Deltorphin 2 - CAS 122752-16-3

Catalog Number: Molecular Weight: 782.88 Molecular Formula: C38H54N8O10 Description: Deltorphin 2, an anion transporting peptid, is a selective peptide agonist for theδ opioid receptor.

Naloxone hydrochloride - CAS 357-08-4

Catalog Number: 357-08-4 Molecular Weight: 363.84 Molecular Formula: C19H21NO4.HCl Description: Naloxone HCl is an opioid inverse agonist drug used to counter the effects of opiate

overdose.

U-54494A hydrochloride - CAS 112465-94-8

Catalog Number: Molecular Weight: 391.77 Molecular Formula: C18H24Cl2N2O.HCl Description: U-54494A hydrochloride is a κ-opioid agonist and a potential NMDA antagonist. U-

54494A hydrochloride is used as an anticonvulsant.

MCOPPB triHydrochloride - CAS 1108147-88-1

Catalog Number: 1108147-88-1 Molecular Weight: 518.01 Molecular Formula: C26H40N4.3HCL Description: The trihydrochloride salt form of MCOPPB, an effective full agonist of nociceptin receptor, could be a good antianxiety agent with few side-effects. pKi: 10.07.

JDTic - CAS 361444-66-8

Catalog Number: 361444-66-8 Molecular Weight: 465.64 Molecular Formula: C28H39N3O3

Description: A 4-phenylpiperidine derivative, for the κ-opioid receptor.

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JDTic dihydrochloride - CAS 785835-79-2

Catalog Number: 785835-79-2 Molecular Weight: 538.55 Molecular Formula: C28H41Cl2N3O3 Description: JDTic dihydrochloride is a highly selective antagonist for the κ-opioid receptor with IC50 value of 0.02nM without affecting the μ- or δ-opioid receptors. It is a 4-phenylpiperidine derivative and distantly structurally related to analgesic drugs such as meperidine and and more closely to the mu opioid antagonist alvimopan. It is structurally distinct

from other kappa antagonists such as . It is more selective and potent for KOR activity than other KOR antagonists. It is shown to block the antinociceptive response of nicotine in the tail-flick test with a dose-dependent manner. It can also block the nicotine withdrawal signs in mice via effecting the expression of a CPA associated with nicotine withdrawal. It is also reported to decrease the number of somatic withdrawal signs in morphine-dependent rats. It may produce antidepressant and anxiolytic effects and may be used in the treatment of addiction to and morphine.

JNJ 20788560 - CAS 825649-28-3

Catalog Number: 825649-28-3 Molecular Weight: 388.51 Molecular Formula: C25H28N2O2 Description: JNJ-20788560 is a delta opioid agonist analgesics. No recent reports of development identified for preclinical development in Inflammatory-pain in USA.

TRV130 HCl - CAS 1401031-39-7

Catalog Number: 1401031-39-7 Molecular Weight: 423.012 Molecular Formula: C22H31ClN2O2S Description: TRV130 is an opioid drug that is under ｅvaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed

by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine.

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Alvimopan monohydrate - CAS 1383577-62-5

Catalog Number: 1383577-62-5 Molecular Weight: 442.55 Molecular Formula: C25H34N2O5 Description: The monohydrate salt form of Alvimopan could be commonly used in postoperative recovery of gastrointestinal for acting as a mu-opioid receptor (PAM-OR) antagonist with IC50: 1.7 nM.

TRV130 - CAS 1401028-24-7

Catalog Number: 1401028-24-7 Molecular Weight: 386.20 Molecular Formula: C22H30N2O2S Description: TRV130 is an oxaspiro compound that has been found to be a μ-opioid receptor G protein ligand and could be used in pain therapy. IC50: 8.1 (pEC50. G protein assay). It is still under Phase III trial for Postoperative pain in USA.

TRV130 Racemate - CAS 1401028-25-8

Catalog Number: 1401028-25-8 Molecular Weight: 386.20 Molecular Formula: C22H30N2O2S Description: The racemate form of TRV130 which is an oxaspiro compound that has been found

to be a μ-opioid receptor G protein ligand and could be used in pain therapy.

BAN ORL 24 dihydrochloride - CAS 1401463-54-4

Catalog Number: Molecular Weight: 506.512 Molecular Formula: C27H37Cl2N3O2 Description: BAN ORL 24 dihydrochloride is a hydrochloride salt form of BAN ORL 24. BAN ORL 24, a spiro-isobenzofuran compound, has been found to be a NOP receptor antagonist and could be used to restrain the reduction of locomotor motions with brain permeability. IC50: 0.27 nM.

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Naloxegol - CAS 854601-70-0

Catalog Number: 854601-70-0 Molecular Weight: 651.78 Molecular Formula: C34H53NO11 Description: Naloxegol is a CYP3A4 enzyme inhibitor. It is also a peripherally-selective opioid antagonist. It is used as the treatment of opioid-induced constipation. lt is a pegylated (polyethylene glycol-modified) derivative of α-naloxol and can be used to reduce opioid-induced

symptoms. lt binds to and blocks mu-opioid receptors in the peripheral nervous system. It would reverse the effects of opiate drugs of abuse if it entered the central nervous system. It was approved in 2014 in adult patients with chronic, non-cancer pain. lt was developed by AstraZeneca, licensed from Nektar Therapeutics. It was approved in 2014 in adult patients with chronic, non-cancer pain. It has been listed.

Cebranopadol - CAS 863513-91-1

Catalog Number: 863513-91-1 Molecular Weight: 378.48 Molecular Formula: C24H27FN2O Description: is a novel first in class compounds with potent agonist activity on opioid receptor like -1(ORL-1) and the well established mu opioid receptor. lt can be obtained from 1,4-Cyclohexanedione Monoethylene Acetal. lt may have the capacity to produce effects and other adverse reactions at sufficiently high doses, a property which

could potentially limit its practical clinical dosage range. It may enhance their effect in certain pain conditions.

GSK1521498 - CAS 1007573-18-3

Catalog Number: 1007573-18-3 Molecular Weight: 402.44 Molecular Formula: C24H20F2N4 Description: GSK-1521498 is a novel μ-Opioid receptor antagonist. It shows to attenuate reward-

driven compulsive behaviours, such as stimulant drug seeking or binge eating in animals and humans. It is mainly used for the treatment of obesity and dependence. It was developed by GlaxoSmithKline and in clinic phase 2.

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Difelikefalin - CAS 1024828-77-0

Catalog Number: 1024828-77-0 Molecular Weight: 679.86 Molecular Formula: C36H53N7O6 Description: is an analgesic opioid peptide acting as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR). It acts as an analgesic by activating KORs on peripheral nerve terminals and KORs expressed by certain immune system cells. It may be useful in the prophylaxis and treatment of pain and associated with a variety of diseases and conditions. It is under development by Cara Therapeutics as an intravenous agent for the treatment of postoperative pain. It lacks the central side effects due to its peripheral selectivity. It is also being investigated for the treatment of pruritus (itching). It has completed phase II clinical trials for postoperative pain and has demonstrated significant and "robust" clinical efficacy, along with being safe and well-tolerated. It is also in phase II clinical trials for uremic pruritus in hemodialysis patients.

LY-190388 - CAS 105496-35-3

Catalog Number: 105496-35-3 Molecular Weight: 615.74 Molecular Formula: C30H41N5O7S

Description: LY-190388 is an μ receptor agonist. It is a penicillamine-containing enkephalin analog and has analgesia effect.

PD-117302 - CAS 111728-01-9

Catalog Number: 111728-01-9 Molecular Weight: 356.52 Molecular Formula: C21H28N2OS Description: PD-117302, a new nonpeptide opioid compound, is a selective kappa-opioid agonist. It has been evaluated in vivo for antinociceptive activity and other effects characteristic of kappa-receptor activation. It also causes naloxone-reversible locomotor impairment and diuresis. It is used as an Anticonvulsants, an Anti-Arrhythmia agent, a Central Nervous System agent and a Cardiovascular agent.

Enadoline hydrochloride - CAS 124439-07-2

Catalog Number: 124439-07-2 Molecular Weight: 432.99 Molecular Formula: C24H33ClN2O3 Description: Enadolineis a potent selective Opioid kappa receptor agonists originated by Pfizer.

However, clinical trials for the treatment of Arrhythmias, Neuroprotection and Pain were discontinued.

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(+)-Igmesine hydrochloride - CAS 130152-35-1

Catalog Number: 130152-35-1 Molecular Weight: 355.94 Molecular Formula: C23H30ClN Description: Igmesine is a selective σ1 receptor ligand (KD = 19.1 nM), with nearly no activity at σ2 receptors (IC50 > 1000 nM). It was developed by Pfizer. Igmesine inhibits the NMDA-induced increase in cGMP in a concentration-dependent manner and IC50 value is approximately 100 nM.

Igmesine can weekly inhibit brain 5-HT uptake in vitro. It exhibits neuroprotective and antidepressant effects. No developments were reported for the treatment of Cognition disorders, Diarrhoea and Major depressive disorder.

Lexanopadol - CAS 1357348-09-4

Catalog Number: 1357348-09-4 Molecular Weight: 364.46 Molecular Formula: C23H25FN2O Description: Lexanopadol is a potent Opioid mu receptor agonist originated by Grunenthal. Lexanopadol is suited for the management of moderate to severe chronic pain, including neuropathic pain. No recent reports of development were identified for phase-I development in

Pain in Germany

CHIR 4531 - CAS 158198-48-2

Catalog Number: 158198-48-2

Molecular Weight: 622.72 Molecular Formula: C36H38N4O6 Description: CHIR 4531, an oligopeptides compound, has been found to be an opioid mu receptor agonist and was once studied in pain therapy.

CP866087 - CAS 519052-02-9

Catalog Number: 519052-02-9 Molecular Weight: 426.57 Molecular Formula: C24H30N2O3S

Description: CP866087 is a selective mu-opioid receptor antagonist.

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Bevenopran - CAS 676500-67-7

Catalog Number: 676500-67-7 Molecular Weight: 386.45 Molecular Formula: C20H26N4O4

Description: is a peripherally selective μ- and δ-opioid receptor antagonist. It is used for the treatment of chronic opioid-induced constipation. It was developed by Cubist Pharmaceuticals and was in clinical phase 3 trial, but now it is terminated.

Odelepran - CAS 676501-25-0

Catalog Number: 676501-25-0 Molecular Weight: 373.43 Molecular Formula: C20H24FN3O3

Description: Odelepran is a opioid receptor antagonist. It is used for the treatment of alcohol dependence. It was developed by Lilly and was in clinical phase 2 trial, but now it is terminated.

LY 123502 - CAS 79561-42-5

Catalog Number: 79561-42-5 Molecular Weight: 666.70 Molecular Formula: C33H39FN6O8

Description: LY 123502 is an opioid agonist, but no detailed information has been published yet.

LY 106737 - CAS 82970-72-7

Catalog Number: 82970-72-7 Molecular Weight: 309.45 Molecular Formula: C21-H27-N-O LY 106737 is phenylpiperidine opioid receptor antagonist, but no detailed information Description: has been published yet.

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