human serotonin

Centanafadine is a dual inhibitor of norepinephrine (NE) dopamine (DA) transporter, also inhibits serotonin transporter (IC50s: 6 nM, 38 nM, and 83 nM for human NE, DA, and serotonin transporter).

Centanafadine hydrochloride (EB-1020 hydrochloride) 是一种去甲肾上腺素(NE) 多巴胺(DA)转运的双抑制剂，还能抑制5-羟色胺(serotonin)转运体。它对人 NE，DA 和5-羟色胺转运体的 IC50值分别为6 nM，38 nM 和 83 nM。

Oleoyl Serotonin 是 hTRPV1 的拮抗剂，IC50（Human TRPV1） 为 2.57 μM。

Ampreloxetine hydrochloride (TD-9855 HCl) 具有抗炎活性，是治疗抑郁症和阿尔茨海默病的潜在化合物。

Trimipramine maleate (Surmontil maleate) 是一种 5-HT 受体拮抗剂，对 5-HT1C、5-HT2和 5-HT1A 受体的 pKi 值分别为 6.39、8.10和 4.66。

Rupatadine(UR-12592,卢帕他定)是一种有效和可口服的PAF和组胺H1受体的双重拮抗剂，Ki 值分别为 0.55 μM 和 0.1 μM，能够缓解过敏症状并抗炎，可用于过敏性鼻炎和慢性荨麻疹。

SB399885 (SB 399885) 是一种有效的脑渗透剂和口服活性 SR-6 拮抗剂。它对 SR-6 的选择性比其他血清素受体高 200 倍（对人重组、天然大鼠和天然人 SR-6 受体的 pKi：分别为 9.11、8.81 和 9.02）。

Frovatriptan succinate hydrate (Frova) 是一种有效、高亲和力、选择性和口服活性的 5-HT1B、HT1D 受体激动剂和中等有效的 5-HT7 受体激动剂，pKi 值分别为 8.6、8.4 和 6.7。它可有效治疗各种偏头痛，包括恶心、呕吐、畏光和畏声等相关症状。

JNJ-18038683 是 5-羟色胺受体 7 拮抗剂，HEK293 细胞中检测出其对大鼠和人类 5-羟色胺受体 7 的pKi 值分别为 8.19和8.20。

ST1936 oxalate 是一种 5-HT6 受体的选择性纳摩尔亲和激动剂，对人5-HT6、5-HT7和 5-HT2B 受体的 Ki 值分别为 13、168 和 245 nM。

PF-04995274 是强效，高亲和力，口服活性血清素 4 受体的部分激动剂。它是可脑渗透的，可用于与阿尔茨海默症相关的认知障碍的研究。

Imipramine (Dimipressin) 是一种具有口服活性的 Fascin1 抑制剂，具有抗抑郁和抗肿瘤活性。Imipramine 抑制 5-羟色胺转运体 （IC50：32 nM），诱导细胞凋亡，诱导 U-87MG 胶质瘤细胞自噬。Imipramine 具有神经保护和免疫调节活性，抑制TNBC细胞的侵袭和迁移，可用于研究乳腺癌和癫痫。

8 Hydroxy PIPAT oxalate 是一种选择性5-HT1A受体激动剂，主要功能是促进肠道肥大细胞释放组胺。该化合物能激活血清素信号通路，在豚鼠和人类肠道制剂中引起肥大细胞脱颗粒现象。此外，8 Hydroxy PIPAT oxalate 可增强组胺的自发释放，这一特性有助于调节胃肠功能，并可能对理解及抑制功能性胃肠道疾病如肠易激综合征等疾病具有研究和治疗的潜在价值。

STOCK3S-30866 是一种针对人类血清素转运体(hSERT)的选择性变构抑制剂。

Loxapine 是 D2DR 和 D4DR 抑制剂和5-羟色胺能受体拮抗剂，是一种抗精神病药物，主要用于治疗精神分裂症。

SB 204741 是一种选择性的5-HT2B 拮抗剂，具有高亲和性，pKi 值为7.1。

SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+ -0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma

N-desmethyl Zolmitriptan (DZT) is an active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist zolmitriptan . DZT is an agonist of 5-HT1B receptors that induces contraction of isolated human cerebral arteries (EC50 = 100 nM).

SCH 38519 is an isochromanequinone fungal metabolite originally isolated from Thermomonospora. It inhibits aggregation induced by thrombin , as well as inhibits serotonin secretion in human platelets (IC50s = 68 and 61 μg/ml, respectively). It inhibits the growth of various Gram-negative and Gram-positive bacteria (mean MICs = 122.1 and 0.92 μg/ml, respectively).

Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters). Reduced haloperidol (0.5 mg kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity.

5-hydroxy-Nω-methyl Tryptamine is a metabolite of serotonin in humans that has also been found in plants. It is an agonist of the 5-HT receptor subtype 5-HT7 (IC50 = 23 pM in a radioligand binding assay). 5-hydroxy-Nω-methyl Tryptamine increases intracellular cyclic AMP production in HEK293 cells expressing 5-HT7 (EC50 = 22 nM). It inhibits serotonin uptake in HEK293 cells expressing human serotonin transporters (IC50 = 490 nM). Elevated levels of urinary 5-hydroxy-Nω-methyl tryptamine have been found in patients with schizophrenia, depression, and epilepsy.

Salvinorin A propionate is a selective partial agonist at κ1-opioid receptors (KOR) with a Ki value of 32.6 nM. It inhibits adenylate cyclase (EC50 = 4.7 nM) in HEK293 cells transfected with human KOR. It is selective for KORs over μ, δ, and ORL-1 opioid receptors and has no effect at serotonin, dopamine, muscarinic, or adrenergic receptors. In mice, salvinorin A propionate (13 μg, i.c.v.) reduces nociceptive responses in a radiant heat tail-flick assay, though not as potently as salvinorin A .

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .

Izuforant (JW1601) (Compound 24) 具有有效的抗炎和止痒活性。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力，IC50值为 9.1 μM。它也是组胺 H4 受体 (H4R) 的口服活性拮抗剂，对人 H4R 的IC50值为 36 nM。